Chemical Biology Consortium Sweden

SAG1.3-derived Frizzled-targeting small molecule compounds.

Grätz L, Turku A, Kozielewicz P, ..., Gmeiner P, Schulte G

J. Biol. Chem. - (-) 110751 [2025-09-22; online 2025-09-22]

Image based subcellular mapping of the protein landscape of SARS-CoV-2 infected cells for target-centric drug repurposing.

Tampere M, H Le T, Asp E, ..., Östling P, Stadler C

Biomed Pharmacother 191 (-) 118447 [2025-08-16; online 2025-08-16]

Chemical Biology Consortium Sweden [Collaborative] Spatial Proteomics [Collaborative]

Genome-wide identification of modulators of Chlamydia trachomatis parasitophorous vacuole stability highlights an important role for sphingolipid supply.

Babu Sait MR, Jachmann LH, Türköz G, ..., Schmierer B, Sixt BS

PLoS Biol. 23 (8) e3003297 [2025-08-00; online 2025-08-12]

CRISPR Functional Genomics [Service] Chemical Biology Consortium Sweden [Service] Integrated Microscopy Technologies Umeå [Technology development] NGI Short read [Service] NGI Stockholm (Genomics Production) [Service] National Genomics Infrastructure [Service]

The low endoribonuclease activity and lack of rNMP preference of human mitochondrial topoisomerase 1 protect against ribonucleotide-dependent deletions

Bader CPJ, Miyazaki-Kasho E, Forslund JME, ..., Wessels M, Wanrooij PH

- 53 (11) - [2025-06-06; online 2025-06-06]

High Content Imaging in Drug Discovery

- - (-) - [2025-04-30; online 2025-04-30]

Chemical Biology Consortium Sweden [Technology development]

Challenging the "Undruggable"─Targeting STAT3 but Identifying Potent TrkA-Targeted Inhibitors.

Iliev P, McCutcheon C, Admas TH, ..., Frank DA, Page BDG

J. Med. Chem. - (-) - [2025-04-17; online 2025-04-17]

Antibacterial compounds against non-growing and intracellular bacteria

Kaldalu N, Bērziņš N, Berglund Fick S, ..., Hauryliuk V, Tenson T

npj Antimicrob Resist 3 (1) - [2025-04-11; online 2025-04-11]

Dual GSK-3β/HDAC Inhibitors Enhance the Efficacy of Macrophages to Control Mycobacterium tuberculosis Infection.

Kalsum S, Xu R, Akber M, ..., Zhou Y, Brighenti S

Biomolecules 15 (4) 550 [2025-04-09; online 2025-04-09]

Design, Synthesis, and Biophysical Characterization of Pyridine Bis‐Quinazoline Derivatives as Selective G‐Quadruplex DNA Stabilizers

Nath Das R, Chorell E

Chem. Eur. J. 31 (21) - [2025-04-09; online 2025-03-05]

The Development of Selective Chemical Probes for Serine Arginine Protein Kinase 3

Hanke D, McCutcheon C, Page BDG

Chem Biol Drug Des 105 (4) - [2025-04-00; online 2025-04-03]

Computational drug repurposing: approaches, evaluation of in silico resources and case studies.

Tanoli Z, Fernández-Torras A, Özcan UO, ..., Carreras-Puigvert J, Aittokallio T

Nat Rev Drug Discov - (-) - [2025-03-18; online 2025-03-18]

Targeting TUBG1 in RB1‐negative tumors

Lindström L, Zhou J, Villoutreix BO, ..., Olsson R, Alvarado‐Kristensson M

The FASEB Journal 39 (5) - [2025-03-15; online 2025-02-28]

Lithography-Free Water Stable Conductive Polymer Nanowires

Hughes D, Mousa AH, Musumeci C, ..., Olsson R, Hjort M

Nano Lett. 25 (8) 3059-3065 [2025-02-26; online 2025-02-13]

Chemical Biology Consortium Sweden [Technology development]

Duplexed CeTEAM drug biosensors reveal determinants of PARP inhibitor selectivity in cells.

Pires MJ, Alam S, Lovric A, ..., Altun M, Valerie NCK

J. Biol. Chem. - (-) 108361 [2025-02-26; online 2025-02-26]

Toward target 2035: EUbOPEN - a public-private partnership to enable & unlock biology in the open.

Tredup C, Ackloo S, Beck H, ..., Arrowsmith CH, Knapp S

RSC Med Chem 16 (2) 457-464 [2025-02-19; online 2024-11-29]

High-content morphological profiling by Cell Painting in 3D spheroids

Ringers C, Holmberg D, Flobak Å, ..., Carreras Puigvert J, Spjuth O

- - (-) - [2025-02-08; online 2025-02-08]

Chemical Biology Consortium Sweden [Technology development]

Nucleobase catalysts for the enzymatic activation of 8-oxoguanine DNA glycosylase 1

Hank EC, D'Arcy-Evans N, Scaletti ER, ..., Helleday T, Michel M

- - (-) - [2025-01-02; online 2025-01-02]

A Rationally Designed Azobenzene Photoswitch for DNA G-Quadruplex Regulation in Live Cells.

Dudek M, López-Pacios L, Sabouri N, ..., Martinez-Fernandez L, Deiana M

Angew. Chem. Int. Ed. Engl. 64 (1) e202413000 [2025-01-02; online 2024-11-06]

Chemogenomic Screening in a Patient‐Derived 3D Fatty Liver Disease Model Reveals the CHRM1‐TRPM8 Axis as a Novel Module for Targeted Intervention

Youhanna S, Kemas AM, Wright SC, ..., Sundström M, Lauschke VM

Adv Sci (Weinh) 12 (3) - [2025-01-00; online 2024-11-28]

Year 2024

Life Science 2.0: reframing the life science sector for 'the benefit on mankind'.

Vallin M, Tomson G, Kampmann B, ..., Wanyenze RK, Ottersen OP

Glob Health Action 17 (1) 2330758 [2024-12-31; online 2024-04-05]

ABHD2 activity is not required for the non-genomic action of progesterone on human sperm

Arnolds O, Carter EM, Edwards M, ..., Tredup C, Gileadi O

- - (-) - [2024-12-18; online 2024-12-18]

Coupling cellular drug-target engagement to downstream pharmacology with CeTEAM.

Valerie NCK, Sanjiv K, Mortusewicz O, ..., Page BDG, Altun M

Nat Commun 15 (1) 10347 [2024-12-06; online 2024-12-06]

Sirtuin inhibitors reduce intracellular growth of M. tuberculosis in human macrophages via modulation of host cell immunity.

Kalsum S, Akber M, Loreti MG, ..., Lerm M, Brighenti S

Sci Rep 14 (1) 28150 [2024-11-15; online 2024-11-15]

Design, synthesis, and in vitro biological evaluation of meta-sulfonamidobenzamide-based antibacterial LpxH inhibitors.

Benediktsdottir A, Sooriyaarachchi S, Cao S, ..., Sandström A, Karlén A

Eur J Med Chem 278 (-) 116790 [2024-11-15; online 2024-08-22]

Patient-derived organoids in precision cancer medicine.

Tong L, Cui W, Zhang B, ..., Si L, Lundqvist A

Med 5 (11) 1351-1377 [2024-11-08; online 2024-09-27]

Loss of heterozygosity of CYP2D6 enhances the sensitivity of hepatocellular carcinomas to talazoparib.

Zhang X, Rameika N, Zhong L, ..., Globisch D, Sjöblom T

EBioMedicine 109 (-) 105368 [2024-11-00; online 2024-10-04]

Dephosphorylation and ion binding in prokaryotic calcium transport.

Prabudiansyah I, Orädd F, Magkakis K, ..., Levantino M, Andersson M

Sci Adv 10 (41) eadp2916 [2024-10-11; online 2024-10-11]

Chemical Biology Consortium Sweden [Service] Cryo-EM [Service]

SETD8 inhibition targets cancer cells with increased rates of ribosome biogenesis.

Murga M, Lopez-Pernas G, Soliva R, ..., Orozco M, Fernández-Capetillo O

Cell Death Dis 15 (9) 694 [2024-09-28; online 2024-09-28]

Chemical Biology Consortium Sweden [Collaborative] Global Proteomics and Proteogenomics [Service]

Harnessing Light for G-Quadruplex Modulation: Dual Isomeric Effects of an Ortho-Fluoroazobenzene Derivative.

Dudek M, López-Pacios L, Sabouri N, ..., Martinez-Fernandez L, Deiana M

J Phys Chem Lett 15 (38) 9757-9765 [2024-09-26; online 2024-09-17]

High-throughput neural stem cell-based drug screening identifies S6K1 inhibition as a selective vulnerability in sonic hedgehog-medulloblastoma.

Zhou L, van Bree N, Boutin L, ..., Falk A, Wilhelm M

Neuro-oncology 26 (9) 1685-1699 [2024-09-05; online 2024-06-11]

A Drug Discovery Pipeline for MAPK/ERK Pathway Inhibitors in Caenorhabditis elegans.

Gorgoń S, Billing O, Eriksson AU, Hemmingsson O

Cancer Res Commun 4 (9) 2454-2462 [2024-09-01; online 2024-08-31]

Heavy-atom-free π-twisted photosensitizers for fluorescence bioimaging and photodynamic therapy.

Sánchez DP, Morice K, Mutovska MG, ..., Cabanetos C, Deiana M

J Mater Chem B 12 (33) 8107-8121 [2024-08-22; online 2024-08-22]

Glycogen synthase kinase 3 inhibition controls Mycobacterium tuberculosis infection.

Peña-Díaz S, Chao JD, Rens C, ..., Pelech S, Av-Gay Y

iScience 27 (8) 110555 [2024-08-16; online 2024-07-20]

AlphaFold accelerated discovery of psychotropic agonists targeting the trace amine-associated receptor 1.

Díaz-Holguín A, Saarinen M, Vo DD, ..., Carlsson J, Svenningsson P

Sci Adv 10 (32) eadn1524 [2024-08-09; online 2024-08-07]

Chemical Biology Consortium Sweden [Service] Drug Discovery and Development [Service]

PrgE: an OB-fold protein from plasmid pCF10 with striking differences to prototypical bacterial SSBs.

Breidenstein A, Lamy A, Bader CP, ..., Wanrooij PH, Berntsson RP

Life Sci. Alliance 7 (8) - [2024-08-00; online 2024-05-29]

Discovery of a novel inhibitor of macropinocytosis with antiviral activity.

Porebski B, Christ W, Corman A, ..., Hühn D, Fernandez-Capetillo O

Mol Ther - (-) - [2024-07-02; online 2024-07-02]

Carboxyl-group compounds activate voltage-gated potassium channels via a distinct mechanism.

Rönnelid O, Elinder F

J. Gen. Physiol. 156 (7) - [2024-07-01; online 2024-06-04]

The anti-leprosy drug clofazimine reduces polyQ toxicity through activation of PPARγ.

Li X, Hernandez I, Koyuncu S, ..., Vilchez D, Fernandez-Capetillo O

EBioMedicine 103 (-) 105124 [2024-05-00; online 2024-05-02]

A phenotypic screening approach to target p60AmotL2-expressing invasive cancer cells.

Fonseca P, Cui W, Struyf N, ..., Östling P, Holmgren L

J. Exp. Clin. Cancer Res. 43 (1) 107 [2024-04-09; online 2024-04-09]

Chemical Biology Consortium Sweden [Collaborative] Global Proteomics and Proteogenomics [Service]

Cancer-associated fibroblasts rewire the estrogen receptor response in luminal breast cancer, enabling estrogen independence.

Reid SE, Pantaleo J, Bolivar P, ..., Seashore-Ludlow B, Pietras K

Oncogene 43 (15) 1113-1126 [2024-04-00; online 2024-02-22]

High Oestrogen receptor alpha expression correlates with adverse prognosis and promotes metastasis in colorectal cancer.

Topi G, Satapathy SR, Ghatak S, ..., Lydrup ML, Sjölander A

Cell Commun Signal 22 (1) 198 [2024-03-28; online 2024-03-28]

Biochemical analysis of the endoribonuclease activity of the human mitochondrial topoisomerase 1

Bader CPJ, Kasho E, Forslund JME, Wessels M, Wanrooij PH

- - (-) - [2024-03-15; online 2024-03-15]

Inhibition of Insulin-Regulated Aminopeptidase by Imidazo [1,5-α]pyridines-Synthesis and Evaluation.

Engen K, Lundbäck T, Yadav A, ..., Hallberg M, Larhed M

Int J Mol Sci 25 (5) - [2024-02-21; online 2024-02-21]

Targeting the Main Protease (Mpro, nsp5) by Growth of Fragment Scaffolds Exploiting Structure-Based Methodologies.

Altincekic N, Jores N, Löhr F, ..., Sreeramulu S, Schwalbe H

ACS Chem. Biol. 19 (2) 563-574 [2024-02-16; online 2024-01-17]

Chemical Biology Consortium Sweden [Service] Swedish NMR Centre [Collaborative]

Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel.

Zhang SM, Paulin CBJ, Shu H, ..., Helleday T, Rudd SG

iScience 27 (2) 108907 [2024-02-16; online 2024-01-13]

Exploring the Dispersion and Electrostatic Components in Arene-Arene Interactions between Ligands and G4 DNA to Develop G4-Ligands.

Andreasson M, Donzel M, Abrahamsson A, ..., Wanrooij S, Chorell E

J. Med. Chem. 67 (3) 2202-2219 [2024-02-08; online 2024-01-19]

Chemical Biology Consortium Sweden [Collaborative] Swedish NMR Centre [Service]

Multiplexed experimental strategies for fragment library screening against challenging drug targets using SPR biosensors.

FitzGerald EA, Vagrys D, Opassi G, ..., de Esch IJP, Danielson UH

SLAS DISCOVERY: Advancing Life Sciences R&D 29 (1) 40-51 [2024-01-00; online 2023-09-14]

Chemical Biology Consortium Sweden [Service] Drug Discovery and Development [Service]

Year 2023

Mitochondrial membrane potential acts as a retrograde signal to regulate cell cycle progression.

Gorospe CM, Carvalho G, Herrera Curbelo A, ..., Niedźwiecka K, Wanrooij PH

Life Sci. Alliance 6 (12) - [2023-12-00; online 2023-09-11]

A multi-strategy antimicrobial discovery approach reveals new ways to combatChlamydia

Ölander M, Vázquez DR, Meier K, ..., Schroeder BO, Sixt BS

- - (-) - [2023-11-30; online 2023-11-30]

Impaired migration and metastatic spread of human melanoma by a novel small molecule targeting the transmembrane domain of death receptor p75NTR

Lopes-Rodrigues V, Nyantakyi SA, Lun X, ..., Senger DL, Ibáñez CF

- - (-) - [2023-11-14; online 2023-11-14]

Modified N-acyl-L-homoserine lactone compounds abrogate Las-dependent quorum-sensing response in human pathogen Pseudomonas aeruginosa.

Ballante F, Turkina MV, Ntzouni M, Magnusson KE, Vikström E

Front Mol Biosci 10 (-) 1264773 [2023-10-16; online 2023-10-16]

Chemical Biology Consortium Sweden [Collaborative] Clinical Genomics [Service] Clinical Genomics Linköping [Service]

Photo-physical characterization of high triplet yield brominated fluoresceins by transient state (TRAST) spectroscopy.

Demirbay B, Baryshnikov G, Haraldsson M, ..., Ågren H, Widengren J

Methods Appl. Fluoresc. 11 (4) - [2023-10-03; online 2023-10-03]

Chemical Biology Consortium Sweden [Collaborative] Swedish Metabolomics Centre [Service]

Inhibiting metabotropic glutamate receptor 5 after stroke restores brain function and connectivity.

Hakon J, Quattromani MJ, Sjölund C, ..., Bauer AQ, Wieloch T

Brain - (-) - [2023-09-01; online 2023-09-01]

The Chlamydia effector CpoS modulates the inclusion microenvironment and restricts the interferon response by acting on Rab35.

Meier K, Jachmann LH, Türköz G, ..., Kroemer G, Sixt BS

MBio 14 (4) e0319022 [2023-08-31; online 2023-08-02]

Loss of CYP2D6 sensitizes hepatocellular carcinomas and neuroblastomas to talazoparib

Sjöblom T, Zhang X, Rameika N, ..., Heim M, Globisch D

- - (-) - [2023-08-21; online 2023-08-21]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Service]

Nucleobase catalysts for the enzymatic activation of 8-oxoguanine DNA glycosylase 1

Hank EC, D'Arcy-Evans N, Wallner O, ..., de Vega M, Michel M

- - (-) - [2023-07-27; online 2023-07-27]

Ciclopirox Ethanolamine Preserves the Immature State of Human HSCs by Mediating Intracellular Iron Content.

Safaee Talkhoncheh M, Baudet A, Ek F, ..., Will B, Larsson J

Blood Adv - (-) - [2023-07-24; online 2023-07-24]

Breeze 2.0: an interactive web-tool for visual analysis and comparison of drug response data.

Potdar S, Ianevski F, Ianevski A, ..., Aittokallio T, Saarela J

Nucleic Acids Res. 51 (W1) W57-W61 [2023-07-05; online 2023-05-14]

Small molecule-mediated disruption of ribosome biogenesis synergizes with FGFR inhibitors to suppress glioma cell growth

Zisi A, Kanellis DC, Moussaud S, ..., Bartek J, Lindström MS

Neuro-oncology 25 (6) 1058-1072 [2023-06-02; online 2022-12-30]

The anti-leprosy drug clofazimine reduces polyQ toxicity through activation of PPAR

Li X, Hernandez I, Häggblad M, ..., Hühn D, Fernandez-Capetillo O

- - (-) - [2023-02-06; online 2023-02-06]

Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1viaa comprehensive screening funnel

Zhang SM, Paulin CBJ, Michel M, ..., Helleday T, Rudd SG

- - (-) - [2023-01-18; online 2023-01-18]

A chemical screen underscores the essential role of STAT1-dependent IFNγ signaling to regulate HLA-I expression in cancer cells.

Barz M, Porebski B, Panshikar P, ..., Hühn D, Fernandez-Capetillo O

MicroPubl Biol 2023 (-) - [2023-01-18; online 2023-01-18]

Optimization of N-Piperidinyl-Benzimidazolone Derivatives as Potent and Selective Inhibitors of 8-Oxo-Guanine DNA Glycosylase 1.

Wallner O, Cázares-Körner A, Scaletti ER, ..., Helleday T, Michel M

ChemMedChem 18 (1) e202200310 [2023-01-03; online 2022-10-13]

Breast cancer patient-derived whole-tumor cell culture model for efficient drug profiling and treatment response prediction.

Chen X, Sifakis EG, Robertson S, ..., Ma R, Hartman J

Proc. Natl. Acad. Sci. U.S.A. 120 (1) e2209856120 [2023-01-03; online 2022-12-27]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Service]

Drug repurposing screens identify compounds that inhibit α-synuclein oligomers' membrane disruption and block antibody interactions

Somavarapu AK, Kleijwegt G, Nagaraj M, ..., Nielsen J, Otzen DE

Chem. Sci. 14 (11) 3030-3047 [2023-00-00; online 2023-00-00]

Year 2022

Monitoring drug-target interactions through target engagement-mediated amplification on arrays and in situ.

Al-Amin RA, Johansson L, Abdurakhmanov E, ..., Lundbäck T, Landegren U

Nucleic Acids Res. 50 (22) e129 [2022-12-09; online 2022-10-04]

Autoimmunity and Serology Profiling [Service] Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Collaborative]

New regulators of the tetracycline‐inducible gene expression system identified by chemical and genetic screens

Colicchia V, Häggblad M, Sirozh O, ..., Hühn D, Fernandez‐Capetillo O

FEBS Open Bio 12 (10) 1896-1908 [2022-10-00; online 2022-09-11]

CRISPR Functional Genomics [Service] Chemical Biology Consortium Sweden [Service]

Enhanced cytotoxicity of a novel family of ATPase inhibitors in colorectal cancer cells with high NAT2 activity

Zhang X, Akcan E, Correia M, ..., Globisch D, Sjöblom T

Biochemical Pharmacology 203 (-) 115184 [2022-09-00; online 2022-09-00]

Glioblastoma CD105+ cells define a SOX2- cancer stem cell-like subpopulation in the pre-invasive niche.

Li J, Ek F, Olsson R, Belting M, Bengzon J

Acta Neuropathol Commun 10 (1) 126 [2022-08-29; online 2022-08-29]

Chemical Biology Consortium Sweden [Collaborative] Clinical Genomics [Service] Clinical Genomics Lund [Service]

Identification of a novel compound that simultaneously impairs the ubiquitin-proteasome system and autophagy.

Giovannucci TA, Salomons FA, Stoy H, ..., Vallin M, Dantuma NP

Autophagy 18 (7) 1486-1502 [2022-07-00; online 2021-11-05]

A high content screening assay for discovery of antimycobacterial compounds based on primary human macrophages infected with virulent Mycobacterium tuberculosis.

Kalsum S, Otrocka M, Andersson B, ..., Lundbäck T, Lerm M

Tuberculosis 135 (-) 102222 [2022-07-00; online 2022-06-16]

Design and development of photoswitchable DFG-Out RET kinase inhibitors.

Xu Y, Gao C, Andreasson M, ..., Andréasson J, Grøtli M

Eur J Med Chem 234 (-) 114226 [2022-04-15; online 2022-03-10]

Small Molecule Screening of Primary Human Acute Myeloid Leukemia Using Co-culture and Multiplexed FACS Analysis.

Baudet A, Hultmark S, Ek F, Magnusson M

BIO-PROTOCOL 12 (6) e4353 [2022-03-20; online 2022-03-20]

High throughput screen in a co-culture model to uncover therapeutic strategies to potentiate the cancer-inhibiting properties of the tumor-stroma in pancreatic cancer

Mason J, Cumming J, Eriksson AU, ..., Chorell E, Öhlund D

- - (-) - [2022-03-13; online 2022-03-13]

Structural Modifications and Biological Evaluations of Rift Valley Fever Virus Inhibitors Identified from Chemical Library Screening.

Islam K, Carlsson M, Enquist PA, ..., Ahlm C, Evander M

ACS Omega 7 (8) 6854-6868 [2022-03-01; online 2022-02-16]

Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses.

Luttens A, Gullberg H, Abdurakhmanov E, ..., Danielson UH, Carlsson J

J. Am. Chem. Soc. 144 (7) 2905-2920 [2022-02-23; online 2022-02-10]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Service] Drug Discovery and Development [Collaborative]

Prolonged estrogen deprivation triggers a broad immunosuppressive phenotype in breast cancer cells

Hühn D, Martí‐Rodrigo P, Mouron S, ..., Carreras‐Puigvert J, Fernandez‐Capetillo O

Mol Oncol 16 (1) 148-165 [2022-01-00; online 2021-08-29]

Year 2021

Structure and ion-release mechanism of PIB-4-type ATPases.

Grønberg C, Hu Q, Mahato DR, ..., Wang K, Gourdon P

Elife 10 (-) - [2021-12-24; online 2021-12-24]

THCz: Small molecules with antimicrobial activity that block cell wall lipid intermediates.

Reithuber E, Wixe T, Ludwig KC, ..., Almqvist F, Mellroth P

Proc. Natl. Acad. Sci. U.S.A. 118 (47) - [2021-11-23; online 2021-11-18]

Monensin induces selective mast cell apoptosis through a secretory granule-mediated pathway.

Maccarana M, Liu J, Lampinen M, ..., Pejler G, Paivandy A

Allergy - (-) - [2021-10-27; online 2021-10-27]

Glioblastoma cytotoxicity conferred through dual disruption of endolysosomal homeostasis by Vacquinol-1.

Kwak D, Hammarström LGJ, Haraldsson M, Ernfors P

Neurooncol Adv 3 (1) vdab152 [2021-10-15; online 2021-10-15]

Inhibition of the ubiquitin-proteasome system by an NQO1-activatable compound.

Giovannucci TA, Salomons FA, Haraldsson M, ..., Johnsen JI, Dantuma NP

Cell Death Dis 12 (10) 914 [2021-10-06; online 2021-10-06]

CRISPR Functional Genomics [Service] Chemical Biology Consortium Sweden [Collaborative] Global Proteomics and Proteogenomics [Service] NGI Stockholm (Genomics Applications) [Service] NGI Stockholm (Genomics Production) [Service] National Genomics Infrastructure [Service]

Design and development of a photoswitchable DFG-out kinase inhibitor.

Xu Y, Gao C, Håversen L, ..., Andréasson J, Grøtli M

Chem. Commun. (Camb.) 57 (78) 10043-10046 [2021-09-30; online 2021-09-30]

Prolonged estrogen deprivation triggers a broad immunosuppressive phenotype in breast cancer cells.

Hühn D, Martí-Rodrigo P, Mouron S, ..., Carreras-Puigvert J, Fernandez-Capetillo O

Mol Oncol - (-) - [2021-08-15; online 2021-08-15]

Identification of Novel Positive Allosteric Modulators of Neurotrophin Receptors for the Treatment of Cognitive Dysfunction.

Dahlström M, Madjid N, Nordvall G, ..., Eriksdotter M, Forsell P

Cells 10 (8) - [2021-07-23; online 2021-07-23]

Inhibition of iduronic acid biosynthesis by ebselen reduces GAG accumulation in MPS-I fibroblasts.

Maccarana M, Tykesson E, Pera EM, ..., Ghiselli G, Li J

Glycobiology - (-) - [2021-06-29; online 2021-06-29]

The chemical compound 'Heatin' stimulates hypocotyl elongation and interferes with the Arabidopsis NIT1-subfamily of nitrilases.

van der Woude L, Piotrowski M, Klaasse G, ..., Smeekens S, van Zanten M

Plant J. 106 (6) 1523-1540 [2021-06-00; online 2021-05-06]

Chemical Biology Consortium Sweden [Service] Swedish Metabolomics Centre [Service]

A chemical screen for modulators of mRNA translation identifies a distinct mechanism of toxicity for sphingosine kinase inhibitors.

Corman A, Kanellis DC, Michalska P, ..., Carreras-Puigvert J, Fernandez-Capetillo O

PLoS Biol. 19 (5) e3001263 [2021-05-00; online 2021-05-25]

Chemical Biology Consortium Sweden; Experiences in academic and industry partnerships – forging a path to translational drug discovery. - Book chapter

Gustavsson A, Chorell E

Burger's Medicinal Chemistry, Drug Discovery and Development, Volumes 1 - 8 Volume 3 (chapter 2) - [2021-04-01]

Chemical Biology Consortium Sweden [Technology development]

Insight into Functional Membrane Proteins by Solution NMR: The Human Bcl-2 Protein-A Promising Cancer Drug Target.

Ul Mushtaq A, Ådén J, Sparrman T, Hedenström M, Gröbner G

Molecules 26 (5) 1467 [2021-03-08; online 2021-03-08]

Chemical Biology Consortium Sweden [Service] Swedish NMR Centre [Service]

Endophilin A2 deficiency protects rodents from autoimmune arthritis by modulating T cell activation.

Norin U, Rintisch C, Meng L, ..., Bäckdahl L, Holmdahl R

Nat Commun 12 (1) 610 [2021-01-27; online 2021-01-27]

Bioinformatics (NBIS) [Collaborative] Bioinformatics Long-term Support WABI [Collaborative] Bioinformatics Support, Infrastructure and Training [Collaborative] Chemical Biology Consortium Sweden [Service] NGI Stockholm (Genomics Applications) NGI Stockholm (Genomics Production) National Genomics Infrastructure

A FabG inhibitor targeting an allosteric binding site inhibits several orthologs from Gram-negative ESKAPE pathogens.

Vella P, Rudraraju RS, Lundbäck T, ..., Schneider G, Schnell R

Bioorg. Med. Chem. 30 (-) 115898 [2021-01-15; online 2020-12-05]

Identification of Small Molecules Blocking the Pseudomonas aeruginosa type III Secretion System Protein PcrV.

Sundin C, Saleeb M, Spjut S, Qin L, Elofsson M

Biomolecules 11 (1) - [2021-01-04; online 2021-01-04]

Chemical Biology Consortium Sweden [Service] Swedish NMR Centre [Service]

Discovery of fragments inducing conformational effects in dynamic proteins using a second-harmonic generation biosensor

FitzGerald EA, Butko MT, Boronat P, ..., Young T, Danielson UH

RSC Adv. 11 (13) 7527-7537 [2021-00-00; online 2021-00-00]

Chemical Biology Consortium Sweden [Service] Drug Discovery and Development

Year 2020

Coupling stabilizers open KV1-type potassium channels.

Silverå Ejneby M, Wallner B, Elinder F

Proc. Natl. Acad. Sci. U.S.A. 117 (43) 27016-27021 [2020-10-27; online 2020-10-13]

Mitigation of the replication of SARS-CoV-2 by nitric oxide in vitro.

Akaberi D, Krambrich J, Ling J, ..., Lennerstrand J, Lundkvist Å

Redox Biol 37 (-) 101734 [2020-10-00; online 2020-09-21]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Service] Drug Discovery and Development [Service] Protein Science Facility (PSF) [Service]

Development of a chemical probe against NUDT15.

Zhang SM, Desroses M, Hagenkort A, ..., Stenmark P, Helleday T

Nat. Chem. Biol. 16 (10) 1120-1128 [2020-10-00; online 2020-07-20]

Chemical Biology Consortium Sweden [Collaborative] Protein Science Facility (PSF) [Service]

Validating Signal Transducer and Activator of Transcription (STAT) Protein-Inhibitor Interactions Using Biochemical and Cellular Thermal Shift Assays.

Attarha S, Reithmeier A, Busker S, Desroses M, Page BDG

ACS Chem. Biol. 15 (7) 1842-1851 [2020-07-17; online 2020-07-02]

Diamond Blackfan anemia is mediated by hyperactive Nemo-like kinase.

Wilkes MC, Siva K, Chen J, ..., Flygare J, Sakamoto KM

Nat Commun 11 (1) 3344 [2020-07-03; online 2020-07-03]

In silico Druggability Assessment of the NUDIX Hydrolase Protein Family as a Workflow for Target Prioritization.

Michel M, Homan EJ, Wiita E, ..., Helleday T, Warpman Berglund U

Front. Chem. 8 (-) 443 [2020-05-29; online 2020-05-29]

Chemical Biology Consortium Sweden [Collaborative] Protein Science Facility (PSF) [Service]

Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.

Popova G, Ladds MJGW, Johansson L, ..., Yngve U, Lain S

J. Med. Chem. 63 (8) 3915-3934 [2020-04-23; online 2020-04-08]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Service]

Exploiting loss of heterozygosity for allele-selective colorectal cancer chemotherapy.

Rendo V, Stoimenov I, Mateus A, ..., Cheong I, Sjöblom T

Nat Commun 11 (1) 1308 [2020-03-11; online 2020-03-11]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Service]

Ribonucleotide reductase inhibitors suppress SAMHD1 ara-CTPase activity enhancing cytarabine efficacy.

Rudd SG, Tsesmetzis N, Sanjiv K, ..., Helleday T, Herold N

EMBO Mol Med 12 (3) e10419 [2020-03-06; online 2020-01-17]

Synthesis, Evaluation and Proposed Binding Pose of Substituted Spiro-Oxindole Dihydroquinazolinones as IRAP Inhibitors.

Engen K, Vanga SR, Lundbäck T, ..., Larhed M, Rosenström U

ChemistryOpen 9 (3) 325-337 [2020-03-00; online 2020-03-02]

Irreversible TrxR1 inhibitors block STAT3 activity and induce cancer cell death.

Busker S, Qian W, Haraldsson M, ..., Tamm KP, Page BDG

Sci Adv 6 (12) eaax7945 [2020-03-00; online 2020-03-20]

Chemical Biology Consortium Sweden [Collaborative] Protein Science Facility (PSF) [Service]

The antimalarial drug amodiaquine stabilizes p53 through ribosome biogenesis stress, independently of its autophagy-inhibitory activity.

Espinoza JA, Zisi A, Kanellis DC, ..., Lindström MS, Bartek J

Cell Death Differ. 27 (2) 773-789 [2020-02-00; online 2019-07-08]

Chemical Biology Consortium Sweden [Service] NGI Stockholm (Genomics Applications) [Service] NGI Stockholm (Genomics Production) [Service] National Genomics Infrastructure [Service]

Perspective on CETSA Literature: Toward More Quantitative Data Interpretation.

Seashore-Ludlow B, Axelsson H, Lundbäck T

SLAS DISCOVERY: Advancing Life Sciences R&D 25 (2) 118-126 [2020-02-00; online 2019-10-30]

Chemical Biology Consortium Sweden [Technology development]

A Chemical Screen Identifies a Link between Lipid Metabolism and mRNA Translation

Corman A, Kanellis DC, Häggblad M, ..., Carreras-Puigvert J, Fernandez-Capetillo O

SSRN Journal - (-) - [2020-00-00; online 2020-00-00]

Year 2019

Chemical Screening Pipeline for Identification of Specific Plant Autophagy Modulators.

Dauphinee AN, Cardoso C, Dalman K, ..., Bozhkov PV, Minina EA

Plant Physiol. 181 (3) 855-866 [2019-11-00; online 2019-09-05]

Discovery and development of substituted thiadiazoles as inhibitors of Staphylococcus aureus Sortase A

Wehrli PM, Uzelac I, Olsson T, ..., Tietze D, Gottfries J

Bioorganic & Medicinal Chemistry 27 (19) 115043 [2019-10-00; online 2019-10-00]

Chemical Biology Consortium Sweden [Service] Glycoproteomics and MS Proteomics [Service] Swedish NMR Centre [Service]

Interaction between VPS35 and RABG3f is necessary as a checkpoint to control fusion of late compartments with the vacuole.

Rodriguez-Furlan C, Domozych D, Qian W, ..., Raikhel NV, Hicks GR

Proc. Natl. Acad. Sci. U.S.A. - (-) - [2019-09-30; online 2019-09-30]

A role for the auxin precursor anthranilic acid in root gravitropism via regulation of PIN-FORMED protein polarity and relocalisation in Arabidopsis.

Doyle SM, Rigal A, Grones P, ..., Novák O, Robert S

New Phytol. 223 (3) 1420-1432 [2019-08-00; online 2019-06-07]

Chemical Biology Consortium Sweden [Service] Swedish Metabolomics Centre [Service]

Computational and Experimental Druggability Assessment of Human DNA Glycosylases.

Michel M, Visnes T, Homan EJ, ..., Warpman Berglund U, Helleday T

ACS Omega 4 (7) 11642-11656 [2019-07-31; online 2019-07-05]

Chemical Biology Consortium Sweden [Collaborative] Swedish NMR Centre [Collaborative]

Development, Optimization, and Validation of a High Throughput Screening Assay for Identification of Tat and Type II Secretion Inhibitors of Pseudomonas aeruginosa.

Massai F, Saleeb M, Doruk T, Elofsson M, Forsberg Å

Front. Cell. Infect. Microbiol. 9 (-) 250 [2019-07-10; online 2019-07-10]

Selective auxin agonists induce specific AUX/IAA protein degradation to modulate plant development.

Vain T, Raggi S, Ferro N, ..., Pauwels L, Robert S

Proc. Natl. Acad. Sci. U.S.A. 116 (13) 6463-6472 [2019-03-26; online 2019-03-08]

Chemical Biology Consortium Sweden [Collaborative] Swedish Metabolomics Centre [Service]

Corticosteroids protect infected cells against mycobacterial killing in vitro.

Tükenmez H, Edström I, Kalsum S, ..., Elofsson M, Larsson C

Biochem. Biophys. Res. Commun. 511 (1) 117-121 [2019-03-26; online 2019-02-14]

Chemical Biology Consortium Sweden [Collaborative] Swedish NMR Centre [Service]

A Phenotypic Screening Assay Identifies Modulators of Diamond Blackfan Anemia.

Siva K, Ek F, Chen J, ..., Lundbäck T, Flygare J

SLAS DISCOVERY: Advancing Life Sciences R&D 24 (3) 304-313 [2019-03-00; online 2019-02-21]

A Chemical Screen Identifies Compounds Limiting the Toxicity of C9ORF72 Dipeptide Repeats

Corman A, Jung B, Häggblad M, ..., Carreras-Puigvert J, Fernandez-Capetillo O

Cell Chem Biol 26 (2) 235-243.e5 [2019-02-00; online 2019-02-00]

Chemical Biology Consortium Sweden [Service] Spatial Proteomics [Service]

Mycobacterium tuberculosis virulence inhibitors discovered by Mycobacterium marinum high-throughput screening.

Tükenmez H, Edström I, Ummanni R, ..., Elofsson M, Larsson C

Sci Rep 9 (1) 26 [2019-01-10; online 2019-01-10]

Year 2018

Sensitive ADAR editing reporter in cancer cells enables high-throughput screening of small molecule libraries

Fritzell K, Xu LD, Otrocka M, Andréasson C, Öhman M

Nucleic Acids Res - (-) - [2018-12-22; online 2018-12-22]

Red Fluorescent Chlamydia trachomatis Applied to Live Cell Imaging and Screening for Antibacterial Agents.

Mojica SA, Eriksson AU, Davis RA, ..., Elofsson M, Gylfe Å

Front Microbiol 9 (-) 3151 [2018-12-18; online 2018-12-18]

Targeting PFKFB3 radiosensitizes cancer cells and suppresses homologous recombination

Gustafsson NMS, Färnegårdh K, Bonagas N, ..., Olin T, Helleday T

Nat Commun 9 (1) - [2018-12-00; online 2018-09-24]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Service] Drug Discovery and Development [Collaborative]

Anti-Rift Valley fever virus activity in vitro, pre-clinical pharmacokinetics and oral bioavailability of benzavir-2, a broad-acting antiviral compound

Islam MK, Strand M, Saleeb M, ..., Elofsson M, Evander M

Sci Rep 8 (1) - [2018-12-00; online 2018-01-31]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Service] Drug Discovery and Development [Service]

A novel derivative of the fungal antimicrobial peptide plectasin is active against Mycobacterium tuberculosis.

Tenland E, Krishnan N, Rönnholm A, ..., Robertson BD, Godaly G

Tuberculosis 113 (-) 231-238 [2018-12-00; online 2018-10-30]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Collaborative]

A drug screening assay on cancer cells chronically adapted to acidosis

Pellegrini P, Serviss JT, Lundbäck T, ..., Linder S, De Milito A

Cancer Cell Int 18 (1) - [2018-12-00; online 2018-09-25]

Using High Content Imaging to Quantify Target Engagement in Adherent Cells.

Axelsson H, Almqvist H, Seashore-Ludlow B

J Vis Exp - (141) - [2018-11-29; online 2018-11-29]

Chemical Biology Consortium Sweden [Technology development]

Quantitative Interpretation of Intracellular Drug Binding and Kinetics Using the Cellular Thermal Shift Assay

Seashore-Ludlow B, Axelsson H, Almqvist H, ..., Jonsson M, Lundbäck T

Biochemistry - (-) - [2018-11-19; online 2018-11-19]

Chemical Biology Consortium Sweden [Technology development]

Small-molecule inhibitor of OGG1 suppresses proinflammatory gene expression and inflammation.

Visnes T, Cázares-Körner A, Hao W, ..., Boldogh I, Helleday T

Science 362 (6416) 834-839 [2018-11-16; online 2018-11-18]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Collaborative] Chemical Proteomics [Collaborative] Drug Discovery and Development [Service] Protein Science Facility (PSF) [Service]

Targeting autophagy by small molecule inhibitors of vacuolar protein sorting 34 (Vps34) improves the sensitivity of breast cancer cells to Sunitinib.

Dyczynski M, Yu Y, Otrocka M, ..., De Milito A, Pokrovskaja Tamm K

Cancer Lett. 435 (-) 32-43 [2018-10-28; online 2018-07-25]

Screening for Inhibitors of Acetaldehyde Dehydrogenase (AdhE) from Enterohemorrhagic Escherichia coli (EHEC).

Zetterström CE, Uusitalo P, Qian W, ..., Grundström C, Elofsson M

SLAS DISCOVERY: Advancing Life Sciences R&D 23 (8) 815-822 [2018-09-00; online 2018-04-09]

The structure-activity relationship of the salicylimide derived inhibitors of UDP-sugar producing pyrophosphorylases.

Decker D, Öberg C, Kleczkowski LA

Plant Signal Behav 13 (8) e1507406 [2018-08-20; online 2018-08-20]

Biaryl sulfonamide motifs up- or down-regulate ion channel activity by activating voltage sensors.

Liin SI, Lund PE, Larsson JE, ..., Wallner B, Elinder F

J. Gen. Physiol. 150 (8) 1215-1230 [2018-08-06; online 2018-07-12]

Identification of inhibitors of Tartrate-resistant acid phosphatase (TRAP/ACP5) activity by small-molecule screening.

Reithmeier A, Lundbäck T, Haraldsson M, ..., Gustavsson AL, Andersson G

Chem Biol Drug Des 92 (1) 1255-1271 [2018-07-00; online 2018-03-30]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Collaborative]

Impact of Dynamically Exposed Polarity on Permeability and Solubility of Chameleonic Drugs Beyond the Rule of 5

Rossi Sebastiano M, Doak BC, Backlund M, ..., Matsson P, Kihlberg J

J. Med. Chem. 61 (9) 4189-4202 [2018-05-10; online 2018-04-02]

Chemical Biology Consortium Sweden [Service] Drug Discovery and Development [Service]

Identification of Poly(ADP-Ribose) Polymerase Macrodomain Inhibitors Using an AlphaScreen Protocol

Ekblad T, Verheugd P, Lindgren AE, ..., Elofsson M, Schüler H

SLAS DISCOVERY: Advancing Life Sciences R&D 23 (4) 353-362 [2018-04-00; online 2018-01-09]

Chemical Biology Consortium Sweden [Service] Protein Science Facility (PSF) [Collaborative]

A DHODH inhibitor increases p53 synthesis and enhances tumor cell killing by p53 degradation blockage.

Ladds MJGW, van Leeuwen IMM, Drummond CJ, ..., McCormack E, Laín S

Nat Commun 9 (1) 1107 [2018-03-16; online 2018-03-16]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Collaborative] Protein Science Facility (PSF) [Service]

In Situ Target Engagement Studies in Adherent Cells

Axelsson H, Almqvist H, Otrocka M, ..., Lundbäck T, Seashore-Ludlow B

ACS Chem. Biol. - (-) - [2018-02-21; online 2018-02-21]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Technology development]

Drug Target Commons: A Community Effort to Build a Consensus Knowledge Base for Drug-Target Interactions.

Tang J, Tanoli ZU, Ravikumar B, ..., Wennerberg K, Aittokallio T

Cell Chem Biol 25 (2) 224-229.e2 [2018-02-15; online 2017-12-21]

Small molecule PGC-1α1 protein stabilizers induce adipocyte Ucp1 expression and uncoupled mitochondrial respiration

Pettersson-Klein AT, Izadi M, Ferreira DMS, ..., Griffin PR, Ruas JL

Mol Metab - (-) - [2018-02-00; online 2018-02-00]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Service]

Targeted NUDT5 inhibitors block hormone signaling in breast cancer cells.

Page BDG, Valerie NCK, Wright RHG, ..., Beato M, Helleday T

Nat Commun 9 (1) 250 [2018-01-17; online 2018-01-17]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Service] Protein Science Facility (PSF) [Service]

Evaluating vacquinol-1 in rats carrying glioblastoma models RG2 and NS1

Ahlstedt J, Förnvik K, Zolfaghari S, ..., Salford LG, Redebrandt HN

Oncotarget - (-) - [2018-01-03; online 2018-01-03]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Collaborative]

Natural product inspired library synthesis - Identification of 2,3-diarylbenzofuran and 2,3-dihydrobenzofuran based inhibitors of Chlamydia trachomatis

Saleeb M, Mojica S, Eriksson AU, ..., Gylfe Å, Elofsson M

European Journal of Medicinal Chemistry 143 (-) 1077-1089 [2018-01-00; online 2018-01-00]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Collaborative]

Year 2017

A chemical screen identifies trifluoperazine as an inhibitor of glioblastoma growth.

Pinheiro T, Otrocka M, Seashore-Ludlow B, ..., Simon A, Kirkham M

Biochem. Biophys. Res. Commun. 494 (3-4) 477-483 [2017-12-16; online 2017-10-21]

Increasing the permeability of Escherichia coli using MAC13243

Muheim C, Götzke H, Eriksson AU, ..., Nørholm MHH, Daley DO

Sci Rep 7 (1) - [2017-12-00; online 2017-12-15]

Motivating students with authentic science experiences: changes in motivation for school science

Hellgren JM, Lindberg S

Research in Science & Technological Education 35 (4) 409-426 [2017-10-02; online 2017-05-03]

Chemical Biology Consortium Sweden [Technology development]

Profiling of in vitro activities of urea-based inhibitors against cysteine synthases from Mycobacterium tuberculosis.

Brunner K, Steiner EM, Reshma RS, ..., Schnell R, Schneider G

Bioorg. Med. Chem. Lett. 27 (19) 4582-4587 [2017-10-01; online 2017-08-19]

Chemical Biology Consortium Sweden [Service] Protein Science Facility (PSF) [Service]

A Drosophila female pheromone elicits species-specific long-range attraction via an olfactory channel with dual specificity for sex and food.

Lebreton S, Borrero-Echeverry F, Gonzalez F, ..., Becher PG, Witzgall P

BMC Biol. 15 (1) 88 [2017-09-29; online 2017-09-29]

Novel spirocyclic systems via multicomponent aza-Diels-Alder reaction.

Llona-Minguez S, Throup A, Steiner E, ..., Jenmalm-Jensen A, Helleday T

Org. Biomol. Chem. 15 (37) 7758-7764 [2017-09-26; online 2017-09-12]

Impact of N-methylation of the substance P 1-7 amide on anti-allodynic effect in mice after peripheral administration.

Skogh A, Lesniak A, Gaugaz FZ, ..., Hallberg M, Sandström A

Eur J Pharm Sci 109 (-) 533-540 [2017-09-05; online 2017-09-05]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Service]

A CRISPR-Cas9 Generated MDCK Cell Line Expressing Human MDR1 Without Endogenous Canine MDR1 (cABCB1): An Improved Tool for Drug Efflux Studies.

Karlgren M, Simoff I, Backlund M, ..., Oswald S, Artursson P

J Pharm Sci 106 (9) 2909-2913 [2017-09-00; online 2017-04-24]

Bioinformatics Support for Computational Resources [Service] Chemical Biology Consortium Sweden [Technology development] Drug Discovery and Development [Technology development] NGI Uppsala (Uppsala Genome Center) [Service] National Genomics Infrastructure [Service]

Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 2: Pyridone- and pyrimidinone-derived systems.

Llona-Minguez S, Häggblad M, Martens U, ..., Scobie M, Helleday T

Bioorg. Med. Chem. Lett. 27 (15) 3219-3225 [2017-08-01; online 2017-06-15]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Service]

Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery

Mateus A, Gordon LJ, Wayne GJ, ..., Hann MM, Artursson P

Proc Natl Acad Sci USA 114 (30) E6231-E6239 [2017-07-25; online 2017-07-12]

Chemical Biology Consortium Sweden [Technology development]

Identification of novel small molecules that inhibit STAT3-dependent transcription and function.

Kolosenko I, Yu Y, Busker S, ..., Page BDG, Grander D

PLoS ONE 12 (6) e0178844 [2017-06-21; online 2017-06-21]

Identification and characterization of inhibitors of UDP-glucose and UDP-sugar pyrophosphorylases for in vivo studies.

Decker D, Öberg C, Kleczkowski LA

Plant J. 90 (6) 1093-1107 [2017-06-00; online 2017-04-13]

High-affinity recognition of the human C-reactive protein independent of phosphocholine.

Yang J, Gustavsson AL, Haraldsson M, ..., Norberg T, Baltzer L

Org. Biomol. Chem. 15 (21) 4644-4654 [2017-05-31; online 2017-05-18]

Chemical Biology Consortium Sweden [Collaborative] Swedish NMR Centre [Service]

Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors.

Llona-Minguez S, Höglund A, Ghassemian A, ..., Scobie M, Helleday T

J. Med. Chem. 60 (10) 4279-4292 [2017-05-25; online 2017-05-16]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Collaborative] Protein Science Facility (PSF) [Service]

dUTPase inhibition augments replication defects of 5-Fluorouracil.

Hagenkort A, Paulin CBJ, Desroses M, ..., Scobie M, Helleday T

Oncotarget 8 (14) 23713-23726 [2017-04-04; online 2017-04-21]

Membrane-Depolarizing Channel Blockers Induce Selective Glioma Cell Death by Impairing Nutrient Transport and Unfolded Protein/Amino Acid Responses.

Niklasson M, Maddalo G, Sramkova Z, ..., Enger PØ, Andäng M

Cancer Res. 77 (7) 1741-1752 [2017-04-01; online 2017-01-13]

Identification of Triazolothiadiazoles as Potent Inhibitors of the dCTP Pyrophosphatase 1.

Llona-Minguez S, Höglund A, Wiita E, ..., Scobie M, Helleday T

J. Med. Chem. 60 (5) 2148-2154 [2017-03-09; online 2017-02-15]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Service]

Targeting SAMHD1 with the Vpx protein to improve cytarabine therapy for hematological malignancies.

Herold N, Rudd SG, Ljungblad L, ..., Helleday T, Schaller T

Nat. Med. 23 (2) 256-263 [2017-02-00; online 2017-01-09]

Chemical Biology Consortium Sweden [Collaborative] Protein Science Facility (PSF) [Service]

Year 2016

Identification of Compounds that Selectively Stabilize Specific G-Quadruplex Structures by Using a Thioflavin T-Displacement Assay as a Tool.

Jamroskovic J, Livendahl M, Eriksson J, Chorell E, Sabouri N

Chemistry 22 (52) 18932-18943 [2016-12-23; online 2016-11-20]

Validation and development of MTH1 inhibitors for treatment of cancer.

Warpman Berglund U, Sanjiv K, Gad H, ..., Scobie M, Helleday T

Ann. Oncol. 27 (12) 2275-2283 [2016-12-00; online 2016-11-08]

Advanced Mass Spectrometry Proteomics [Collaborative] Bioinformatics (NBIS) [Collaborative] Bioinformatics Support and Infrastructure [Collaborative] Bioinformatics Support, Infrastructure and Training [Collaborative] Chemical Biology Consortium Sweden [Collaborative] Chemical Proteomics [Service] Clinical Proteomics Mass spectrometry [Collaborative] Drug Discovery and Development [Collaborative]

Structural and conformational determinants of macrocycle cell permeability

Over B, Matsson P, Tyrchan C, ..., Duvall JR, Kihlberg J

Nat Chem Biol 12 (12) 1065-1074 [2016-12-00; online 2016-10-17]

Chemical Biology Consortium Sweden [Technology development]

Early Perspective: Microplate Applications of the Cellular Thermal Shift Assay (CETSA)

Seashore-Ludlow B, Lundbäck T

J Biomol Screen 21 (10) 1019-1033 [2016-12-00; online 2016-07-20]

Chemical Biology Consortium Sweden [Technology development]

Identification and Characterization of Novel Compounds Blocking Shiga Toxin Expression in Escherichia coli O157:H7.

Huerta-Uribe A, Marjenberg ZR, Yamaguchi N, ..., Gally DL, Roe AJ

Front Microbiol 7 (-) 1930 [2016-11-30; online 2016-11-30]

Discovery of Selective Inhibitors Targeting Acetylcholinesterase 1 from Disease-Transmitting Mosquitoes.

Engdahl C, Knutsson S, Ekström F, Linusson A

J. Med. Chem. 59 (20) 9409-9421 [2016-10-27; online 2016-09-07]

Auxotrophy-based High Throughput Screening assay for the identification of Bacillus subtilis stringent response inhibitors.

Andresen L, Varik V, Tozawa Y, ..., Tenson T, Hauryliuk V

Sci Rep 6 (-) 35824 [2016-10-24; online 2016-10-24]

Aryl Sulfonamide Inhibitors of Insulin-Regulated Aminopeptidase Enhance Spine Density in Primary Hippocampal Neuron Cultures.

Diwakarla S, Nylander E, Grönbladh A, ..., Chai SY, Hallberg M

ACS Chem Neurosci 7 (10) 1383-1392 [2016-10-19; online 2016-08-08]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Collaborative]

The Oncolytic Efficacy and in Vivo Pharmacokinetics of [2-(4-Chlorophenyl)quinolin-4-yl](piperidine-2-yl)methanol (Vacquinol-1) Are Governed by Distinct Stereochemical Features.

Hammarström LG, Harmel RK, Granath M, ..., Lehmann F, Ernfors P

J. Med. Chem. 59 (18) 8577-8592 [2016-09-22; online 2016-09-09]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Collaborative]

Design and Synthesis of 2,2'-Diindolylmethanes to Selectively Target Certain G-Quadruplex DNA Structures.

Livendahl M, Jamroskovic J, Ivanova S, ..., Sabouri N, Chorell E

Chemistry 22 (37) 13004-13009 [2016-09-05; online 2016-07-20]

Inhibitors of the Cysteine Synthase CysM with Antibacterial Potency against Dormant Mycobacterium tuberculosis.

Brunner K, Maric S, Reshma RS, ..., Schnell R, Schneider G

J. Med. Chem. 59 (14) 6848-6859 [2016-07-28; online 2016-07-13]

Chemical Biology Consortium Sweden [Collaborative] Protein Science Facility (PSF) [Service]

Tumor acidosis enhances cytotoxic effects and autophagy inhibition by salinomycin on cancer cell lines and cancer stem cells.

Pellegrini P, Dyczynski M, Sbrana FV, ..., Kharaziha P, De Milito A

Oncotarget 7 (24) 35703-35723 [2016-06-14; online 2016-06-02]

Modifications of the 7-Hydroxyl Group of the Transthyretin Ligand Luteolin Provide Mechanistic Insights into Its Binding Properties and High Plasma Specificity.

Nilsson L, Larsson A, Begum A, ..., Sauer-Eriksson AE, Olofsson A

PLoS ONE 11 (4) e0153112 [2016-04-06; online 2016-04-06]

Identification of Drug-Like Inhibitors of Insulin-Regulated Aminopeptidase Through Small-Molecule Screening.

Engen K, Rosenström U, Axelsson H, ..., Lundbäck T, Larhed M

Assay Drug Dev Technol 14 (3) 180-193 [2016-04-00; online 2016-04-15]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Service]

High-Throughput Screening Using a Whole-Cell Virus Replication Reporter Gene Assay to Identify Inhibitory Compounds against Rift Valley Fever Virus Infection.

Islam MK, Baudin M, Eriksson J, ..., Ahlm C, Evander M

J Biomol Screen 21 (4) 354-362 [2016-04-00; online 2016-01-15]

Binding to and Inhibition of Insulin-Regulated Aminopeptidase by Macrocyclic Disulfides Enhances Spine Density.

Diwakarla S, Nylander E, Grönbladh A, ..., Chai SY, Hallberg M

Mol. Pharmacol. 89 (4) 413-424 [2016-04-00; online 2016-01-16]

CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil.

Almqvist H, Axelsson H, Jafari R, ..., Lundbäck T, Nordlund P

Nat Commun 7 (-) 11040 [2016-03-24; online 2016-03-24]

Chemical Biology Consortium Sweden [Collaborative] Protein Science Facility (PSF) [Service]

Thiazolino 2-Pyridone Amide Inhibitors of Chlamydia trachomatis Infectivity.

Good JA, Silver J, Núñez-Otero C, ..., Bergström S, Almqvist F

J. Med. Chem. 59 (5) 2094-2108 [2016-03-10; online 2016-02-22]

Mechanistic Modeling of Pitavastatin Disposition in Sandwich-Cultured Human Hepatocytes: A Proteomics-Informed Bottom-Up Approach

Vildhede A, Mateus A, Khan EK, ..., Artursson P, Kjellsson MC

Drug Metab. Dispos. 44 (4) 505-516 [2016-02-26; online 2016-02-03]

Chemical Biology Consortium Sweden [Technology development]

Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1.

Llona-Minguez S, Höglund A, Jacques SA, ..., Scobie M, Helleday T

J. Med. Chem. 59 (3) 1140-1148 [2016-02-11; online 2016-01-27]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Collaborative] Protein Science Facility (PSF) [Service]

Direct Measurement of Intracellular Compound Concentration by RapidFire Mass Spectrometry Offers Insights into Cell Permeability

Gordon LJ, Allen M, Artursson P, ..., Wayne GJ, West A

J Biomol Screen 21 (2) 156-164 [2016-02-00; online 2015-09-03]

Chemical Biology Consortium Sweden [Technology development]

Complete Knockout of Endogenous Mdr1 ( Abcb1 ) in MDCK Cells by CRISPR-Cas9

Simoff I, Karlgren M, Backlund M, ..., Matsson P, Artursson P

Journal of Pharmaceutical Sciences 105 (2) 1017-1021 [2016-02-00; online 2016-02-00]

Chemical Biology Consortium Sweden [Technology development] NGI Uppsala (Uppsala Genome Center) [Service] National Genomics Infrastructure [Service]

Year 2015

Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo.

Caraballo R, Larsson M, Nilsson SK, ..., Enquist P, Elofsson M

Eur J Med Chem 103 (-) 191-209 [2015-10-20; online 2015-09-12]

Dibenzocyclooctadiene lignans from Schisandra spp. selectively inhibit the growth of the intracellular bacteria Chlamydia pneumoniae and Chlamydia trachomatis.

Hakala E, Hanski L, Uvell H, ..., Elofsson M, Vuorela PM

J. Antibiot. 68 (10) 609-614 [2015-10-00; online 2015-05-07]

Virtual Screening for Transition State Analogue Inhibitors of IRAP Based on Quantum Mechanically Derived Reaction Coordinates

Svensson F, Engen K, Lundbäck T, Larhed M, Sköld C

J. Chem. Inf. Model. 55 (9) 1984-1993 [2015-09-28; online 2015-09-28]

Tandem Benzophenone Amino Pyridines, Potent and Selective Inhibitors of Human Leukotriene C4 Synthase

Kleinschmidt TK, Haraldsson M, Basavarajappa D, ..., Lindbom L, Haeggstrom JZ

Journal of Pharmacology and Experimental Therapeutics 355 (1) 108-116 [2015-09-08; online 2015-08-17]

Design, Synthesis and Inhibitory Activity of Photoswitchable RET Kinase Inhibitors

Ferreira R, Nilsson JR, Solano C, Andréasson J, Grøtli M

Sci Rep 5 (1) - [2015-09-00; online 2015-05-06]

Structural Basis for the Specificity of Human NUDT16 and Its Regulation by Inosine Monophosphate

Trésaugues L, Lundbäck T, Welin M, ..., Gräslund S, Nordlund P

PLoS ONE 10 (6) e0131507 [2015-06-29; online 2015-06-29]

Chemical Biology Consortium Sweden [Collaborative] Protein Science Facility (PSF)

CETSA: a target engagement assay with potential to transform drug discovery

Jensen AJ, Molina DM, Lundbäck T

Future Medicinal Chemistry 7 (8) 975-978 [2015-06-00; online 2015-06-00]

Crystal structures of the kinase domain of the sulfate-activating complex in Mycobacterium tuberculosis.

Poyraz Ö, Brunner K, Lohkamp B, ..., Schnell R, Schneider G

PLoS ONE 10 (3) e0121494 [2015-03-25; online 2015-03-25]

Chemical Biology Consortium Sweden [Collaborative] Protein Science Facility (PSF)

Preclinical characterization of acyl sulfonimidamides: potential carboxylic acid bioisosteres with tunable properties.

Borhade SR, Svensson R, Brandt P, ..., Arvidsson PI, Sandström A

ChemMedChem 10 (3) 455-460 [2015-03-00; online 2015-01-30]

Novel high-throughput screening method for identification of fungal dimorphism blockers.

Stylianou M, Uvell H, Lopes JP, ..., Elofsson M, Urban CF

J Biomol Screen 20 (2) 285-291 [2015-02-00; online 2014-10-05]

Year 2014

Inhibitory Activity of the Isoflavone Biochanin A on Intracellular Bacteria of Genus Chlamydia and Initial Development of a Buccal Formulation

Hanski L, Genina N, Uvell H, ..., Sandler N, Vuorela PM

PLoS ONE 9 (12) e115115 [2014-12-16; online 2014-12-16]

Exploration and pharmacokinetic profiling of phenylalanine based carbamates as novel substance p 1-7 analogues.

Fransson R, Nordvall G, Bylund J, ..., Hallberg M, Sandström A

ACS Med Chem Lett 5 (12) 1272-1277 [2014-12-11; online 2014-10-29]

Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles.

Lampa A, Alogheli H, Ehrenberg AE, ..., Karlén A, Sandström A

Bioorg. Med. Chem. 22 (23) 6595-6615 [2014-12-01; online 2014-12-03]

Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides.

Borhade SR, Rosenström U, Sävmarker J, ..., Larhed M, Hallberg M

ChemistryOpen 3 (6) 256-263 [2014-12-00; online 2014-11-21]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Collaborative]

Microwave Heated Flow Synthesis of Spiro-oxindole Dihydroquinazolinone Based IRAP Inhibitors

Engen K, Sävmarker J, Rosenström U, ..., Jenmalm-Jensen A, Larhed M

Org. Process Res. Dev. 18 (11) 1582-1588 [2014-11-21; online 2014-10-16]

Design of a general-purpose European compound screening library for EU-OPENSCREEN.

Horvath D, Lisurek M, Rupp B, ..., Quintana J, Frank R

ChemMedChem 9 (10) 2309-2326 [2014-10-00; online 2014-07-15]

Chemical Biology Consortium Sweden [Technology development]

Controversies inASSAY and Drug Development Technologies: A Focus on Assessing Irreproducibility

Glickman JF, Lundbäck T, Napper AD, ..., Zaman GJR, Osada H

ASSAY and Drug Development Technologies 12 (8) 443-451 [2014-10-00; online 2014-10-00]

Chemical Biology Consortium Sweden [Technology development]

The cellular thermal shift assay for evaluating drug target interactions in cells

Jafari R, Almqvist H, Axelsson H, ..., Nordlund P, Molina DM

Nat Protoc 9 (9) 2100-2122 [2014-08-07; online 2014-08-07]

Chemical Biology Consortium Sweden [Technology development]

Identification of a small molecule that stabilizes lipoprotein lipase in vitro and lowers triglycerides in vivo.

Larsson M, Caraballo R, Ericsson M, ..., Nilsson SK, Olivecrona G

Biochem. Biophys. Res. Commun. 450 (2) 1063-1069 [2014-07-25; online 2014-07-02]

Screening for inhibition of Vibrio cholerae VipA-VipB interaction identifies small-molecule compounds active against type VI secretion.

Sun K, Bröms J, Lavander M, ..., Elofsson M, Sjöstedt A

Antimicrob. Agents Chemother. 58 (7) 4123-4130 [2014-07-00; online 2014-05-07]

Hepatic uptake of atorvastatin: influence of variability in transporter expression on uptake clearance and drug-drug interactions.

Vildhede A, Karlgren M, Svedberg EK, ..., Norén A, Artursson P

Drug Metab. Dispos. 42 (7) 1210-1218 [2014-07-00; online 2014-05-05]

CXCR4 Antagonists: A Screening Strategy for Identification of Functionally Selective Ligands.

Castaldo C, Benicchi T, Otrocka M, ..., Varrone M, Porcari V

J Biomol Screen 19 (6) 859-869 [2014-07-00; online 2014-03-14]

Immunomodulatory activity of commonly used drugs on Fc-receptor-mediated human natural killer cell activation.

Theorell J, Gustavsson AL, Tesi B, ..., Lundbäck T, Bryceson YT

Cancer Immunol. Immunother. 63 (6) 627-641 [2014-06-00; online 2014-03-30]

Structure and inhibition of mouse leukotriene C4 synthase.

Niegowski D, Kleinschmidt T, Ahmad S, ..., Rinaldo-Matthis A, Haeggström JZ

PLoS ONE 9 (5) e96763 [2014-05-08; online 2014-05-08]

Chemical Biology Consortium Sweden [Service] Protein Science Facility (PSF)

N-acylated derivatives of sulfamethoxazole and sulfafurazole inhibit intracellular growth of Chlamydia trachomatis.

Marwaha S, Uvell H, Salin O, ..., Elofsson M, Gylfe A

Antimicrob. Agents Chemother. 58 (5) 2968-2971 [2014-05-00; online 2014-02-26]

Vulnerability of glioblastoma cells to catastrophic vacuolization and death induced by a small molecule.

Kitambi SS, Toledo EM, Usoskin D, ..., Hammarström LGJ, Ernfors P

Cell 157 (2) 313-328 [2014-04-10; online 2014-03-25]

MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool.

Gad H, Koolmeister T, Jemth A, ..., Berglund UW, Helleday T

Nature 508 (7495) 215-221 [2014-04-10; online 2014-04-02]

Chemical Biology Consortium Sweden [Collaborative] Drug Discovery and Development [Collaborative] Protein Science Facility (PSF)

A high-throughput cell-based method to predict the unbound drug fraction in the brain.

Mateus A, Matsson P, Artursson P

J. Med. Chem. 57 (7) 3005-3010 [2014-04-10; online 2014-03-20]

Chemical Biology Consortium Sweden [Technology development]

Syntheses and biological evaluation of 2-amino-3-acyl-tetrahydrobenzothiophene derivatives; antibacterial agents with antivirulence activity.

Dang HT, Chorell E, Uvell H, ..., Hultgren SJ, Almqvist F

Org. Biomol. Chem. 12 (12) 1942-1956 [2014-03-28; online 2014-02-17]

Impact of stereospecific intramolecular hydrogen bonding on cell permeability and physicochemical properties.

Over B, McCarren P, Artursson P, ..., Duvall JR, Kihlberg J

J. Med. Chem. 57 (6) 2746-2754 [2014-03-27; online 2014-02-15]

Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2-P1' Region.

Lampa AK, Bergman SM, Gustafsson SS, ..., Karlén A, Sandström A

ACS Med Chem Lett 5 (3) 249-254 [2014-03-13; online 2013-08-02]

Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket.

Gising J, Belfrage AK, Alogheli H, ..., Larhed M, Sandström A

J. Med. Chem. 57 (5) 1790-1801 [2014-03-13; online 2013-03-23]

2′-(Z)-Cinnamoylsalicortin: A novel salicinoid isolated from Populus tremula

Keefover-Ring K, Carlsson M, Albrectsen BR

Phytochemistry Letters 7 (-) 212-216 [2014-02-00; online 2014-02-00]

Isolation and characterization of anti-adenoviral secondary metabolites from marine actinobacteria.

Strand M, Carlsson M, Uvell H, ..., Wadell G, Almqvist F

Mar Drugs 12 (2) 799-821 [2014-01-28; online 2014-01-28]

A luminescence-based assay of UDP-sugar producing pyrophosphorylases

Decker D, Lindberg S, Eriksson J, Kleczkowski LA

Anal. Methods 6 (1) 57-61 [2014-00-00; online 2014-00-00]

Year 2013

Structure-activity relationships of synthetic cordycepin analogues as experimental therapeutics for African trypanosomiasis.

Vodnala SK, Lundbäck T, Yeheskieli E, ..., Hammarström LG, Rottenberg ME

J. Med. Chem. 56 (24) 9861-9873 [2013-12-27; online 2013-12-10]

Statistical molecular design: a tool to follow up hits from small-molecule screening.

Lindgren AE, Larsson A, Linusson A, Elofsson M

Methods Mol. Biol. 1056 (-) 169-188 [2013-12-07; online 2013-12-07]

Chemical Biology Consortium Sweden [Technology development]

The resveratrol tetramer (-)-hopeaphenol inhibits type III secretion in the gram-negative pathogens Yersinia pseudotuberculosis and Pseudomonas aeruginosa.

Zetterström CE, Hasselgren J, Salin O, ..., Sundin C, Elofsson M

PLoS ONE 8 (12) e81969 [2013-12-04; online 2013-12-04]

Combined in vitro-in vivo approach to assess the hepatobiliary disposition of a novel oral thrombin inhibitor.

Matsson EM, Eriksson UG, Palm JE, ..., Schützer K, Lennernäs H

Mol. Pharm. 10 (11) 4252-4262 [2013-11-04; online 2013-10-02]

Divergent structure-activity relationships of structurally similar acetylcholinesterase inhibitors.

Andersson CD, Forsgren N, Akfur C, ..., Ekström F, Linusson A

J. Med. Chem. 56 (19) 7615-7624 [2013-10-10; online 2013-08-30]

Ebsulfur is a benzisothiazolone cytocidal inhibitor targeting the trypanothione reductase of Trypanosoma brucei.

Lu J, Vodnala SK, Gustavsson AL, ..., Rottenberg ME, Holmgren A

J. Biol. Chem. 288 (38) 27456-27468 [2013-09-20; online 2013-07-29]

Structure-Guided Design of Novel Thiazolidine Inhibitors ofO-Acetyl Serine Sulfhydrylase from Mycobacterium tuberculosis

Poyraz Ö, Jeankumar VU, Saxena S, ..., Sriram D, Schneider G

J. Med. Chem. 56 (16) 6457-6466 [2013-08-22; online 2013-08-22]

An Integratedin VitroModel for Simultaneous Assessment of Drug Uptake, Metabolism, and Efflux

Neve EPA, Artursson P, Ingelman-Sundberg M, Karlgren M

Mol. Pharmaceutics 10 (8) 3152-3163 [2013-08-05; online 2013-08-05]

Design of a highly selective and potent class of non-planar estrogen receptor β agonists.

Sundén H, Ma JN, Hansen LK, ..., Burstein ES, Olsson R

ChemMedChem 8 (8) 1283-1294 [2013-08-00; online 2013-06-19]

Computational Prospecting for Drug–Transporter Interactions

Matsson P, Artursson P

Clin Pharmacol Ther 94 (1) 30-32 [2013-07-00; online 2013-04-02]

Chemical Biology Consortium Sweden [Technology development]

Constrained H-Phe-Phe-NH2 analogues with high affinity to the substance P 1-7 binding site and with improved metabolic stability and cell permeability.

Fransson R, Sköld C, Kratz JM, ..., Hallberg M, Sandström A

J. Med. Chem. 56 (12) 4953-4965 [2013-06-27; online 2013-06-06]

Rapid Measurement of Intracellular Unbound Drug Concentrations

Mateus A, Matsson P, Artursson P

Mol. Pharmaceutics 10 (6) 2467-2478 [2013-06-03; online 2013-06-03]

Chemical Biology Consortium Sweden [Technology development]

The value of selected in vitro and in silico methods to predict acute oral toxicity in a regulatory context: results from the European Project ACuteTox.

Prieto P, Kinsner-Ovaskainen A, Stanzel S, ..., Zurbano MJ, Kopp-Schneider A

Toxicol In Vitro 27 (4) 1357-1376 [2013-06-00; online 2012-08-28]

Optimizing Solubility and Permeability of a Biopharmaceutics Classification System (BCS) Class 4 Antibiotic Drug Using Lipophilic Fragments Disturbing the Crystal Lattice

Tehler U, Fagerberg JH, Svensson R, ..., Artursson P, Bergström CAS

J. Med. Chem. 56 (6) 2690-2694 [2013-03-28; online 2013-03-28]

Chemical Biology Consortium Sweden [Technology development]

Population pharmacokinetic modeling and deconvolution of enantioselective absorption of eflornithine in the rat

Johansson CC, Gennemark P, Artursson P, ..., Ashton M, Jansson-Löfmark R

J Pharmacokinet Pharmacodyn 40 (1) 117-128 [2013-02-00; online 2013-01-10]

In vitro and in vivo activities of 2-aminopyrazines and 2-aminopyridines in experimental models of human African trypanosomiasis.

Vodnala SK, Lundbäck T, Sjöberg B, ..., Rottenberg ME, Hammarström LGJ

Antimicrob. Agents Chemother. 57 (2) 1012-1018 [2013-02-00; online 2012-12-21]

The A-CD analogue of 16β,17α-estriol is a potent and highly selective estrogen receptor β agonist

Sauvée C, Schäfer A, Sundén H, ..., Burstein ES, Olsson R

Med. Chem. Commun. 4 (11) 1439 [2013-00-00; online 2013-00-00]

Year 2012

Berg L, Niemiec MS, Qian W, ..., Ekström F, Linusson A

Angew. Chem. Int. Ed. Engl. 51 (51) 12716-12720 [2012-12-14; online 2012-11-20]

2-[4,5-Difluoro-2-(2-fluorobenzoylamino)-benzoylamino]benzoic acid, an antiviral compound with activity against acyclovir-resistant isolates of herpes simplex virus types 1 and 2.

Strand M, Islam K, Edlund K, ..., Elofsson M, Wadell G

Antimicrob. Agents Chemother. 56 (11) 5735-5743 [2012-11-00; online 2012-08-22]

Discovery of Ligands for ADP-Ribosyltransferases via Docking-Based Virtual Screening

Andersson CD, Karlberg T, Ekblad T, ..., Schüler H, Linusson A

J. Med. Chem. 55 (17) 7706-7718 [2012-09-13; online 2012-09-13]

Chemical Biology Consortium Sweden [Service] Protein Science Facility (PSF)

The novel tyrosine kinase inhibitor AKN-028 has significant antileukemic activity in cell lines and primary cultures of acute myeloid leukemia

Eriksson A, Hermanson M, Wickström M, ..., Parrow V, Höglund M

Blood Cancer J 2 (8) e81 [2012-08-00; online 2012-08-00]

Evidence-based approach to assess passive diffusion and carrier-mediated drug transport

Di L, Artursson P, Avdeef A, ..., Lennernäs H, Sugano K

Drug Discovery Today 17 (15-16) 905-912 [2012-08-00; online 2012-08-00]

Chemical Biology Consortium Sweden [Technology development]

Design, synthesis and evaluation of triazole functionalized ring-fused 2-pyridones as antibacterial agents.

Bengtsson C, Lindgren AEG, Uvell H, Almqvist F

Eur J Med Chem 54 (-) 637-646 [2012-08-00; online 2012-07-04]

Small molecule screening for inhibitors of the YopH phosphatase of Yersinia pseudotuberculosis.

Eriksson J, Grundström C, Sauer-Eriksson AE, ..., Wolf-Watz H, Elofsson M

Adv. Exp. Med. Biol. 954 (-) 357-363 [2012-07-12; online 2012-07-12]

Ethanol effects on apparent solubility of poorly soluble drugs in simulated intestinal fluid.

Fagerberg JH, Al-Tikriti Y, Ragnarsson G, Bergström CAS

Mol. Pharm. 9 (7) 1942-1952 [2012-07-02; online 2012-06-02]

A non-peptide receptor inhibitor with selectivity for one of the neutrophil formyl peptide receptors, FPR 1

Çevik-Aras H, Kalderén C, Jenmalm Jensen A, ..., Dahlgren C, Forsman H

Biochemical Pharmacology 83 (12) 1655-1662 [2012-06-00; online 2012-06-00]

Classification of Inhibitors of Hepatic Organic Anion Transporting Polypeptides (OATPs): Influence of Protein Expression on Drug–Drug Interactions

Karlgren M, Vildhede A, Norinder U, ..., Haglund U, Artursson P

J. Med. Chem. 55 (10) 4740-4763 [2012-05-24; online 2012-05-15]

Derivatives of 8-hydroxyquinoline--antibacterial agents that target intra- and extracellular Gram-negative pathogens.

Enquist P, Gylfe A, Hägglund U, ..., Sundin C, Elofsson M

Bioorg. Med. Chem. Lett. 22 (10) 3550-3553 [2012-05-15; online 2012-04-25]

Synthesis, biological evaluation, and structure-activity relationships of 2-[2-(benzoylamino)benzoylamino]benzoic acid analogues as inhibitors of adenovirus replication.

Öberg CT, Strand M, Andersson EK, ..., Wadell G, Elofsson M

J. Med. Chem. 55 (7) 3170-3181 [2012-04-12; online 2012-03-01]

Syntheses of pseudoceramines A-D and a new synthesis of spermatinamine, bromotyrosine natural products from marine sponges.

Hillgren JM, Oberg CT, Elofsson M

Org. Biomol. Chem. 10 (6) 1246-1254 [2012-02-14; online 2011-12-20]

In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions.

Karlgren M, Ahlin G, Bergström CA, ..., Palm J, Artursson P

Pharm. Res. 29 (2) 411-426 [2012-02-00; online 2011-08-23]

Chemical Biology Consortium Sweden [Technology development]

Year 2011

Targeting acetylcholinesterase: identification of chemical leads by high throughput screening, structure determination and molecular modeling.

Berg L, Andersson CD, Artursson E, ..., Linusson A, Ekström F

PLoS ONE 6 (11) e26039 [2011-11-30; online 2011-11-30]

Pseudoceramines A-D, new antibacterial bromotyrosine alkaloids from the marine sponge Pseudoceratina sp.

Yin S, Davis RA, Shelper T, ..., Sundin C, Quinn RJ

Org. Biomol. Chem. 9 (19) 6755-6760 [2011-10-07; online 2011-08-19]

Structural features determining the intestinal epithelial permeability and efflux of novel HIV-1 protease inhibitors.

Lazorova L, Hubatsch I, Ekegren JK, ..., Larhed M, Artursson P

J Pharm Sci 100 (9) 3763-3772 [2011-09-00; online 2011-04-15]

Identification of Bacterial Target Proteins for the Salicylidene Acylhydrazide Class of Virulence-blocking Compounds

Wang D, Zetterström CE, Gabrielsen M, ..., Elofsson M, Roe AJ

J. Biol. Chem. 286 (34) 29922-29931 [2011-08-26; online 2011-07-01]

Synthesis and application of a bromomethyl substituted scaffold to be used for efficient optimization of anti-virulence activity.

Chorell E, Bengtsson C, Sainte-Luce Banchelin T, ..., Hultgren SJ, Almqvist F

Eur J Med Chem 46 (4) 1103-1116 [2011-04-00; online 2011-01-21]

Year 2010

Small-molecule screening using a whole-cell viral replication reporter gene assay identifies 2-{[2-(benzoylamino)benzoyl]amino}-benzoic acid as a novel antiadenoviral compound.

Andersson EK, Strand M, Edlund K, ..., Mei Y, Wadell G

Antimicrob. Agents Chemother. 54 (9) 3871-3877 [2010-09-00; online 2010-06-30]