Drug Discovery and Development (DDD)

An Adaptable Antibody‐Based Platform for Flexible Synthetic Peptide Delivery Built on Agonistic CD40 Antibodies

Eltahir M, Laurén I, Lord M, ..., Persson H, Mangsbo SM

Advanced Therapeutics - (-) 2200008 [2022-06-14; online 2022-06-14]

Drug Discovery and Development (DDD) [Collaborative]

Broad-spectrum antidote discovery by untangling the reactivation mechanism of nerve agent inhibited acetylcholinesterase.

Lindgren C, Forsgren N, Hoster N, ..., Ekström F, Linusson A

Chemistry - (-) - [2022-04-14; online 2022-04-14]

Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress.

Bonagas N, Gustafsson NMS, Henriksson M, ..., Homan EJ, Helleday T

Nat Cancer 3 (2) 156-172 [2022-02-00; online 2022-02-28]

Drug Discovery and Development (DDD) [Collaborative]

Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors.

Brem J, Panduwawala T, Hansen JU, ..., Walsh TR, Schofield CJ

Nat Chem 14 (1) 15-24 [2022-01-00; online 2021-12-13]

Year 2021

Melphalan flufenamide inhibits osteoclastogenesis by suppressing proliferation of monocytes.

Byrgazov K, Lind T, Rasmusson AJ, ..., Larsson R, Fryknäs M

Bone Rep 15 (-) 101098 [2021-12-00; online 2021-06-07]

Fed-batch production assessment of a tetravalent bispecific antibody: A case study on piggyBac stably transfected HEK293 cells.

Napoleone A, Laurén I, Linkgreim T, ..., Lord M, Mangsbo S

N Biotechnol 65 (-) 9-19 [2021-11-25; online 2021-07-15]

Drug Discovery and Development (DDD) [Collaborative]

Selection and structural characterization of anti-TREM2 scFvs that reduce levels of shed ectodomain.

Szykowska A, Chen Y, Smith TB, ..., Burgess-Brown NA, Bullock AN

Structure 29 (11) 1241-1252.e5 [2021-11-04; online 2021-07-06]

Drug Discovery and Development (DDD) [Collaborative]

ENABLE: an engine for European antibacterial drug discovery and development.

Olliver M, Griestop L, Hughes D, ..., Vingsbo Lundberg C, Karlén A

Nat Rev Drug Discov 20 (6) 407-408 [2021-06-00; online 2021-05-06]

Drug Discovery and Development (DDD) [Collaborative]

Discovery of an Allosteric Ligand Binding Site in SMYD3 Lysine Methyltransferase.

Talibov VO, Fabini E, FitzGerald EA, ..., Del Rio A, Danielson UH

ChemBioChem 22 (9) 1597-1608 [2021-05-04; online 2021-02-11]

N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.

Wannberg J, Gising J, Lindman J, ..., Hallberg M, Larhed M

Bioorg. Med. Chem. 29 (-) 115859 [2021-01-01; online 2020-11-07]

Drug Discovery and Development (DDD) [Collaborative]

A Tribute to Professor Per Artursson - Scientist, Explorer, Mentor, Innovator, and Giant in Pharmaceutical Research.

Matsson P, Baranczewski P, Giacomini KM, ..., Charman WN, Bergström CAS

J Pharm Sci 110 (1) 2-11 [2021-01-00; online 2020-10-21]

Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Collaborative]

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 (CBCS) [Service] Drug Discovery and Development (DDD)

Year 2020

Rational Design of Azastatin as a Potential ADC Payload with Reduced Bystander Killing.

Hartmann RW, Fahrner R, Shevshenko D, ..., Lehmann F, Odell LR

ChemMedChem 15 (24) 2500-2512 [2020-12-15; online 2020-10-16]

Generation and validation of recombinant antibodies to study human aminoacyl-tRNA synthetases.

Preger C, Wigren E, Ossipova E, ..., Gräslund S, Persson H

J. Biol. Chem. 295 (41) 13981-13993 [2020-10-09; online 2020-08-14]

Autoimmunity and Serology Profiling [Service] Drug Discovery and Development (DDD) [Collaborative]

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 Compute and Storage [Service] Drug Discovery and Development (DDD) [Service]

Mebendazole is unique among tubulin-active drugs in activating the MEK-ERK pathway.

Andersson CR, Selvin T, Blom K, ..., Nygren P, Larsson R

Sci Rep 10 (1) 13124 [2020-08-04; online 2020-08-04]

Descriptive Proteome Analysis to Investigate Context-Dependent Treatment Responses to OXPHOS Inhibition in Colon Carcinoma Cells Grown as Monolayer and Multicellular Tumor Spheroids.

Steinmetz J, Senkowski W, Lengqvist J, ..., Fryknäs M, Kultima K

ACS Omega 5 (28) 17242-17254 [2020-07-21; online 2020-07-06]

Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Service]

A Patient-Derived Cell Atlas Informs Precision Targeting of Glioblastoma.

Johansson P, Krona C, Kundu S, ..., Marino S, Nelander S

Cell Rep 32 (2) 107897 [2020-07-14; online 2020-07-16]

Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Service]

High content drug screening for Fanconi anemia therapeutics.

Montanuy H, Camps-Fajol C, Carreras-Puigvert J, ..., Minguillón J, Surrallés J

Orphanet J Rare Dis 15 (1) 170 [2020-06-30; online 2020-06-30]

Comprehensive chemical proteomics for target deconvolution of the redox active drug auranofin.

Saei AA, Gullberg H, Sabatier P, ..., Arnér ESJ, Zubarev RA

Redox Biol 32 (-) 101491 [2020-05-00; online 2020-03-03]

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]

Establishing Trypanosoma cruzi farnesyl pyrophosphate synthase as a viable target for biosensor driven fragment-based lead discovery.

Opassi G, Nordström H, Lundin A, ..., Klebe G, Danielson UH

Protein Sci. 29 (4) 991-1003 [2020-04-00; online 2020-02-07]

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 Compute and Storage [Service] Chemical Biology Consortium Sweden (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Service]

Tumor localized agonistic anti-CD40 therapy and beyond.

Eltahir M, Persson H, Mangsbo S

Expert Opin Biol Ther 20 (3) 215-217 [2020-03-00; online 2020-01-10]

Drug Discovery and Development (DDD) [Collaborative]

Estimating Detection Limits of Potentiometric DNA Sensors Using Surface Plasmon Resonance Analyses.

Xu X, Makaraviciute A, Abdurakhmanov E, ..., Nyholm L, Zhang Z

ACS Sens. 5 (1) 217-224 [2020-01-24; online 2019-12-23]

Drug Discovery and Development (DDD) [Technology development]

Year 2019

Structural Changes of Mercaptohexanol Self-Assembled Monolayers on Gold and Their Influence on Impedimetric Aptamer Sensors.

Xu X, Makaraviciute A, Kumar S, ..., Nyholm L, Zhang Z

Anal. Chem. 91 (22) 14697-14704 [2019-11-19; online 2019-11-07]

Drug Discovery and Development (DDD) [Technology development]

A Cell-Free Approach Based on Phospholipid Characterization for Determination of the Cell Specific Unbound Drug Fraction (f u,cell).

Treyer A, Walday S, Boriss H, Matsson P, Artursson P

Pharm. Res. 36 (12) 178 [2019-11-07; online 2019-11-07]

Drug Discovery and Development (DDD) [Technology development]

Methyl sulfonamide substituents improve the pharmacokinetic properties of bicyclic 2-pyridone based Chlamydia trachomatis inhibitors.

Kulén M, Núñez-Otero C, Cairns AG, ..., Gylfe Å, Almqvist F

Med. Chem. Commun. 10 (11) 1966-1987 [2019-11-01; online 2019-10-17]

Mesenchymal transition and increased therapy resistance of glioblastoma cells is related to astrocyte reactivity.

Niklasson M, Bergström T, Jarvius M, ..., Segerman B, Segerman A

J. Pathol. 249 (3) 295-307 [2019-11-00; online 2019-08-31]

Inhibition of translation termination by small molecules targeting ribosomal release factors.

Ge X, Oliveira A, Hjort K, ..., Sanyal S, Åqvist J

Sci Rep 9 (1) 15424 [2019-10-28; online 2019-10-28]

Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Service]

N-Trifluoromethylthiolated Sulfonimidamides and Sulfoximines: Anti-microbial, Anti-mycobacterial, and Cytotoxic Activity.

Thota N, Makam P, Rajbongshi KK, ..., Naicker T, Arvidsson PI

ACS Med Chem Lett 10 (10) 1457-1461 [2019-10-10; online 2019-09-11]

Drug Discovery and Development (DDD) [Technology development]

A novel tumor spheroid model identifies selective enhancement of radiation by an inhibitor of oxidative phosphorylation.

Karlsson H, Senkowski W, Fryknäs M, ..., Larsson R, Nygren P

Oncotarget 10 (51) 5372-5382 [2019-09-03; online 2019-09-03]

Circulating Levels of Interferon Regulatory Factor-5 Associates With Subgroups of Systemic Lupus Erythematosus Patients.

Idborg H, Zandian A, Ossipova E, ..., Svenungsson E, Jakobsson PJ

Front Immunol 10 (-) 1029 [2019-05-17; online 2019-05-17]

Affinity Proteomics Stockholm [Collaborative] Drug Discovery and Development (DDD) [Collaborative]

Mebendazole-induced M1 polarisation of THP-1 macrophages may involve DYRK1B inhibition.

Blom K, Rubin J, Berglund M, ..., Nygren P, Larsson R

BMC Res Notes 12 (1) 234 [2019-04-22; online 2019-04-22]

Improved predictions of time-dependent drug-drug interactions by determination of cytosolic drug concentrations.

Filppula AM, Parvizi R, Mateus A, Baranczewski P, Artursson P

Sci Rep 9 (1) 5850 [2019-04-10; online 2019-04-10]

Drug Discovery and Development (DDD) [Technology development]

Synthesis of Sulfonimidamide-Based Amino Acid Building Blocks with Orthogonal Protecting Groups

Chinthakindi PK, Benediktsdottir A, Ibrahim A, ..., Chen Y, Sandström A

Eur. J. Org. Chem. 2019 (5) 1045-1057 [2019-02-07; online 2019-01-02]

Drug Discovery and Development (DDD) [Technology development]

Targeted Analysis of Serum Proteins Encoded at Known Inflammatory Bowel Disease Risk Loci.

Drobin K, Assadi G, Hong MG, ..., D'Amato M, Halfvarson J

Inflamm Bowel Dis 25 (2) 306-316 [2019-01-10; online 2018-10-26]

Affinity Proteomics Stockholm [Collaborative] Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Collaborative]

A Series of Analogues to the AT 2R Prototype Antagonist C38 Allow Fine Tuning of the Previously Reported Antagonist Binding Mode.

Isaksson R, Lindman J, Wannberg J, ..., Gising J, Larhed M

ChemistryOpen 8 (1) 114-125 [2019-01-00; online 2019-01-24]

Drug Discovery and Development (DDD) [Collaborative]

Year 2018

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 Compute and Storage [Service] Chemical Biology Consortium Sweden (CBCS) [Service] Drug Discovery and Development (DDD) [Collaborative]

Publisher Correction: 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) - [2018-12-00; online 2018-05-22]

Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Service]

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 Compute and Storage [Service] Chemical Biology Consortium Sweden (CBCS) [Service] Drug Discovery and Development (DDD) [Service]

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 Compute and Storage [Service] Chemical Biology Consortium Sweden (CBCS) [Collaborative] Chemical Proteomics [Collaborative] Drug Discovery and Development (DDD) [Service] Protein Science Facility (PSF) [Service]

Combination of phage and Gram-positive bacterial display of human antibody repertoires enables isolation of functional high affinity binders.

Hu FJ, Volk AL, Persson H, ..., Uhlen M, Rockberg J

N Biotechnol 45 (-) 80-88 [2018-10-25; online 2017-08-01]

Drug Discovery and Development (DDD) [Technology development]

The downfall of TBA-354 - a possible explanation for its neurotoxicity via mass spectrometric imaging.

Ntshangase S, Shobo A, Kruger HG, ..., Govender T, Baijnath S

Xenobiotica 48 (9) 938-944 [2018-09-00; online 2017-10-13]

Drug Discovery and Development (DDD) [Collaborative]

Sulfonimidamides: Synthesis and Applications in Preparative Organic Chemistry

Nandi GC, Arvidsson PI

Adv. Synth. Catal. 360 (16) 2976-3001 [2018-08-17; online 2018-05-25]

Drug Discovery and Development (DDD) [Technology development]

Sulfonyl Fluorides (SFs): More Than Click Reagents?

Chinthakindi PK, Arvidsson PI

Eur. J. Org. Chem. 2018 (27-28) 3648-3666 [2018-08-01; online 2018-07-06]

Drug Discovery and Development (DDD) [Technology development]

Proteome‐wide analysis of phospho‐regulated PDZ domain interactions

Sundell GN, Arnold R, Ali M, ..., Chi CN, Ivarsson Y

Mol. Syst. Biol. 14 (8) e8129 [2018-08-00; online 2018-08-20]

Drug Discovery and Development (DDD) [Service] NGI Uppsala (SNP&SEQ Technology Platform) [Service] National Genomics Infrastructure [Service]

An imidazole based H-Phe-Phe-NH 2 peptidomimetic with anti-allodynic effect in spared nerve injury mice

Skogh A, Lesniak A, Sköld C, ..., Hallberg M, Sandström A

Bioorganic & Medicinal Chemistry Letters 28 (14) 2446-2450 [2018-08-00; online 2018-08-00]

Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Service]

Mebendazole stimulates CD14+ myeloid cells to enhance T-cell activation and tumour cell killing.

Rubin J, Mansoori S, Blom K, ..., Nygren P, Larsson R

Oncotarget 9 (56) 30805-30813 [2018-07-20; online 2018-07-20]

In Vitro Evolution of Antibodies Inspired by In Vivo Evolution

Persson H, Kirik U, Thörnqvist L, ..., Levander F, Ohlin M

Front Immunol 9 (-) - [2018-06-21; online 2018-06-21]

Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [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 (CBCS) [Service] Drug Discovery and Development (DDD) [Service]

Autophagic flux blockage by accumulation of weakly basic tenovins leads to elimination of B-Raf mutant tumour cells that survive vemurafenib

Ladds MJGW, Pastor-Fernández A, Popova G, ..., Bhatia R, Laín S

PLoS ONE 13 (4) e0195956 [2018-04-23; online 2018-04-23]

Introduction of Intrinsic Kinetics of Protein-Ligand Interactions and Their Implications for Drug Design.

Linkuvienė V, Talibov VO, Danielson UH, Matulis D

J. Med. Chem. 61 (6) 2292-2302 [2018-03-22; online 2018-03-02]

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

Lipids Shape the Electron Acceptor-Binding Site of the Peripheral Membrane Protein Dihydroorotate Dehydrogenase

Costeira-Paulo J, Gault J, Popova G, ..., Marklund EG, Landreh M

Cell Chem Biol 25 (3) 309-317.e4 [2018-03-00; online 2018-03-00]

Drug Discovery and Development (DDD) [Collaborative]

Advancing the immunoaffinity platform AFFIRM to targeted measurements of proteins in serum in the pg/ml range.

Säll A, Corbee D, Vikström S, ..., Persson H, Waldemarson S

PLoS ONE 13 (2) e0189116 [2018-02-13; online 2018-02-13]

Drug Discovery and Development (DDD) [Technology development]

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 Compute and Storage [Service] Chemical Biology Consortium Sweden (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Service]

A convenient transesterification method for synthesis of AT2 receptor ligands with improved stability in human liver microsomes

Wannberg J, Isaksson R, Bremberg U, ..., Hallberg M, Larhed M

Bioorganic & Medicinal Chemistry Letters 28 (3) 519-522 [2018-02-00; online 2018-02-00]

Drug Discovery and Development (DDD) [Collaborative]

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 Compute and Storage [Service] Drug Discovery and Development (DDD) [Service] Protein Science Facility (PSF) [Service]

Clofazimine protects against Mycobacterium tuberculosis dissemination in the central nervous system following aerosol challenge in a murine model.

Baijnath S, Moodley C, Ngcobo B, ..., Pym A, Govender T

International Journal of Antimicrobial Agents 51 (1) 77-81 [2018-01-00; online 2017-08-24]

Drug Discovery and Development (DDD) [Collaborative]

Synthesis of novel 1,2,4-thiadiazinane 1,1-dioxides via three component SuFEx type reaction

Khumalo MF, Akpan ED, Chinthakindi PK, ..., Naicker T, Arvidsson PI

RSC Adv. 8 (65) 37503-37507 [2018-00-00; online 2018-00-00]

Drug Discovery and Development (DDD) [Technology development]

An unexpected re-arrangement of the antibiotic carbapenem core to new 1,4-diazepin-5-one scaffolds

Peters BK, Razuwika R, Samipillai M, ..., Govender T, Naicker T

RSC Adv. 8 (1) 190-193 [2018-00-00; online 2018-00-00]

Drug Discovery and Development (DDD) [Collaborative]

Year 2017

Targeting tumor cells based on Phosphodiesterase 3A expression.

Nazir M, Senkowski W, Nyberg F, ..., Larsson R, Fryknäs M

Exp. Cell Res. 361 (2) 308-315 [2017-12-15; online 2017-10-26]

Towards repositioning of quinacrine for treatment of acute myeloid leukemia - Promising synergies and in vivo effects.

Eriksson A, Chantzi E, Fryknäs M, ..., Höglund M, Larsson R

Leuk Res 63 (-) 41-46 [2017-12-00; online 2017-10-28]

A comprehensive structural, biochemical and biological profiling of the human NUDIX hydrolase family

Carreras-Puigvert J, Zitnik M, Jemth AS, ..., Zupan B, Helleday T

Nat Commun 8 (1) - [2017-12-00; online 2017-11-16]

BioImage Informatics [Collaborative] Drug Discovery and Development (DDD) [Collaborative] Protein Science Facility (PSF) [Service]

Bliss and Loewe interaction analyses of clinically relevant drug combinations in human colon cancer cell lines reveal complex patterns of synergy and antagonism.

Kashif M, Andersson C, Mansoori S, ..., Nygren P, Gustafsson MG

Oncotarget 8 (61) 103952-103967 [2017-11-28; online 2017-10-19]

Antibody Heavy Chain Variable Domains of Different Germline Gene Origins Diversify through Different Paths

Kirik U, Persson H, Levander F, Greiff L, Ohlin M

Front Immunol 8 (-) - [2017-11-13; online 2017-11-13]

Bioinformatics Support and Infrastructure [Collaborative] Bioinformatics Support, Infrastructure and Training [Collaborative] Drug Discovery and Development (DDD) [Collaborative]

Institutional profile: the national Swedish academic drug discovery & development platform at SciLifeLab.

Arvidsson PI, Sandberg K, Sakariassen KS

Future Sci. OA 3(2), FSO176 (2) - [2017-10-30; online 2017-04-07]

Drug Discovery and Development (DDD) [Technology development]

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [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 Compute and Storage [Service] Chemical Biology Consortium Sweden (CBCS) [Technology development] Drug Discovery and Development (DDD) [Technology development] NGI Uppsala (Uppsala Genome Center) [Service] National Genomics Infrastructure [Service]

Importance of N- and C-terminal residues of substance P 1-7 for alleviating allodynia in mice after peripheral administration.

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

Eur J Pharm Sci 106 (-) 345-351 [2017-08-30; online 2017-06-03]

Drug Discovery and Development (DDD) [Collaborative]

Diverse heterocyclic scaffolds as dCTP pyrophosphatase 1 inhibitors. Part 1: Triazoles, triazolopyrimidines, triazinoindoles, quinoline hydrazones and arylpiperazines.

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

Bioorg. Med. Chem. Lett. 27 (16) 3897-3904 [2017-08-15; online 2017-06-16]

Drug Discovery and Development (DDD) [Collaborative]

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Service]

The anticancer effect of mebendazole may be due to M1 monocyte/macrophage activation via ERK1/2 and TLR8-dependent inflammasome activation.

Blom K, Senkowski W, Jarvius M, ..., Nygren P, Larsson R

Immunopharmacol Immunotoxicol 39 (4) 199-210 [2017-08-00; online 2017-05-04]

Lansoprazole-sulfide, pharmacokinetics of this promising anti-tuberculous agent

Mdanda S, Baijnath S, Shobo A, ..., Naicker T, Govender T

Biomedical Chromatography - (-) e4035 [2017-07-13; online 2017-07-13]

Drug Discovery and Development (DDD) [Collaborative]

Structure-metabolism-relationships in the microsomal clearance of piperazin-1-ylpyridazines.

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

Med. Chem. Commun. 8 (7) 1553-1560 [2017-07-01; online 2017-07-04]

Drug Discovery and Development (DDD) [Collaborative]

Global Kinetic Mechanism of Microsomal Glutathione Transferase 1 and Insights into Dynamic Enzyme Activation.

Spahiu L, Ålander J, Ottosson-Wadlund A, ..., Armstrong RN, Morgenstern R

Biochemistry 56 (24) 3089-3098 [2017-06-20; online 2017-06-09]

Drug Discovery and Development (DDD) [Collaborative]

Synthetic approaches to radiochemical probes for imaging of bacterial infections

Dutta J, Naicker T, Ebenhan T, ..., Arvidsson PI, Govender T

European Journal of Medicinal Chemistry 133 (-) 287-308 [2017-06-00; online 2017-06-00]

Drug Discovery and Development (DDD) [Collaborative]

On the bridge over the translational valley of death: interview with Per I Arvidsson.

Arvidsson PI

Future Science OA 3 (2) FSO183 [2017-06-00; online 2017-04-10]

Drug Discovery and Development (DDD) [Technology development]

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Collaborative]

Mechanistic characterization of a copper containing thiosemicarbazone with potent antitumor activity.

Karlsson H, Fryknäs M, Strese S, ..., Larsson R, Nygren P

Oncotarget 8 (18) 30217-30234 [2017-05-02; online 2017-04-19]

Glioblastoma Cell Malignancy and Drug Sensitivity Are Affected by the Cell of Origin.

Jiang Y, Marinescu VD, Xie Y, ..., Nelander S, Uhrbom L

Cell Rep 19 (5) 1080-1081 [2017-05-02; online 2017-05-04]

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

Gad H, Koolmeister T, Jemth AS, ..., Scobie M, Ulrika Warpman Berglund &Thomas Helleday

Nature 544 (7651) 508 [2017-04-26; online 2017-04-28]

Sulfonimidamides in Medicinal and Agricultural Chemistry

Chinthakindi PK, Naicker T, Thota N, ..., Kruger HG, Arvidsson PI

Angew. Chem. Int. Ed. 56 (15) 4100-4109 [2017-04-03; online 2017-02-23]

Drug Discovery and Development (DDD) [Technology development]

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Service]

Antibody Validation by Immunoprecipitation Followed by Mass Spectrometry Analysis.

Persson H, Preger C, Marcon E, Lengqvist J, Gräslund S

Methods Mol. Biol. 1575 (-) 175-187 [2017-03-04; online 2017-03-04]

Intracellular drug bioavailability: a new predictor of system dependent drug disposition.

Mateus A, Treyer A, Wegler C, ..., Matsson P, Artursson P

Sci Rep 7 (-) 43047 [2017-02-22; online 2017-02-22]

Crystal Structure of the Emerging Cancer Target MTHFD2 in Complex with a Substrate-Based Inhibitor.

Gustafsson R, Jemth AS, Gustafsson NM, ..., Helleday T, Stenmark P

Cancer Res. 77 (4) 937-948 [2017-02-15; online 2016-11-29]

Drug Discovery and Development (DDD) [Collaborative]

A Synthesis of “Dual Warhead” β-Aryl Ethenesulfonyl Fluorides and One-Pot Reaction to β-Sultams

Chinthakindi PK, Govender KB, Kumar AS, ..., Naicker T, Arvidsson PI

Org. Lett. 19 (3) 480-483 [2017-02-03; online 2017-01-11]

Drug Discovery and Development (DDD) [Technology development]

In vitro and in vivo anti-leukemic activity of the peptidase-potentiated alkylator melflufen in acute myeloid leukemia.

Strese S, Hassan SB, Velander E, ..., Larsson R, Gullbo J

Oncotarget 8 (4) 6341-6352 [2017-01-24; online 2016-12-16]

Year 2016

Clonal Variation in Drug and Radiation Response among Glioma-Initiating Cells Is Linked to Proneural-Mesenchymal Transition.

Segerman A, Niklasson M, Haglund C, ..., Segerman B, Westermark B

Cell Rep 17 (11) 2994-3009 [2016-12-13; online 2016-12-16]

Drug Discovery and Development (DDD) [Service] NGI Uppsala (SNP&SEQ Technology Platform) [Service] National Genomics Infrastructure [Service]

Iron chelators target both proliferating and quiescent cancer cells.

Fryknäs M, Zhang X, Bremberg U, ..., Linder S, Larsson R

Sci Rep 6 (-) 38343 [2016-12-07; online 2016-12-07]

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

Large-Scale Gene Expression Profiling Platform for Identification of Context-Dependent Drug Responses in Multicellular Tumor Spheroids.

Senkowski W, Jarvius M, Rubin J, ..., Larsson R, Fryknäs M

Cell Chem Biol 23 (11) 1428-1438 [2016-11-17; online 2016-10-27]

Drug Discovery and Development (DDD) [Service] Tissue Profiling [Service]

Case-specific potentiation of glioblastoma drugs by pterostilbene.

Schmidt L, Baskaran S, Johansson P, ..., Krona C, Nelander S

Oncotarget 7 (45) 73200-73215 [2016-11-08; online 2016-10-01]

Drug Discovery and Development (DDD) [Collaborative]

Tryptophan Metabolism Along the Kynurenine Pathway Downstream of Toll-like Receptor Stimulation in Peripheral Monocytes.

Orhan F, Bhat M, Sandberg K, ..., Erhardt S, Schwieler L

Scand. J. Immunol. 84 (5) 262-271 [2016-11-00; online 2016-10-27]

Drug Discovery and Development (DDD) [Collaborative]

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Collaborative]

Open for collaboration: an academic platform for drug discovery and development at SciLifeLab.

Arvidsson PI, Sandberg K, Forsberg-Nilsson K

Drug Discov. Today 21 (10) 1690-1698 [2016-10-00; online 2016-07-05]

Drug Discovery and Development (DDD) [Technology development]

Generation and analyses of human synthetic antibody libraries and their application for protein microarrays.

Säll A, Walle M, Wingren C, ..., Borrebaeck CAK, Persson H

Protein Eng. Des. Sel. 29 (10) 427-437 [2016-10-00; online 2016-09-01]

Drug Discovery and Development (DDD) [Technology development] Protein Science Facility (PSF) [Collaborative]

Biophysics in drug discovery: impact, challenges and opportunities.

Renaud JP, Chung CW, Danielson UH, ..., Hubbard RE, Nar H

Nat Rev Drug Discov 15 (10) 679-698 [2016-10-00; online 2016-08-16]

Drug Discovery and Development (DDD) [Technology development]

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Collaborative]

The peroxisome proliferator-activated receptor α agonist, AZD4619, induces alanine aminotransferase-1 gene and protein expression in human, but not in rat hepatocytes: Correlation with serum ALT levels.

Thulin P, Bamberg K, Buler M, Dahl B, Glinghammar B

Int. J. Mol. Med. 38 (3) 961-968 [2016-09-00; online 2016-07-20]

Drug Discovery and Development (DDD) [Collaborative]

Repeated LPS Injection Induces Distinct Changes in the Kynurenine Pathway in Mice.

Larsson MK, Faka A, Bhat M, ..., Schwieler L, Erhardt S

Neurochem. Res. 41 (9) 2243-2255 [2016-09-00; online 2016-05-10]

Drug Discovery and Development (DDD) [Collaborative]

Enantioselective Organocatalyzed Transformations of β-Ketoesters.

Govender T, Arvidsson PI, Maguire GE, Kruger HG, Naicker T

Chem. Rev. 116 (16) 9375-9437 [2016-08-24; online 2016-07-28]

Drug Discovery and Development (DDD) [Collaborative]

Neuroprotective potential of Linezolid: a quantitative and distribution study via mass spectrometry.

Baijnath S, Shobo A, Bester LA, ..., Naicker T, Govender T

J. Mol. Histol. 47 (4) 429-435 [2016-08-00; online 2016-06-22]

Drug Discovery and Development (DDD) [Collaborative]

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Service]

A Facile Synthesis of NODASA-Functionalized Peptide

Naicker T, Albericio F, Dutta J, ..., Kruger H, Govender T

Synlett 27 (11) 1685-1688 [2016-03-30; online 2016-03-30]

Drug Discovery and Development (DDD) [Collaborative]

On-Water Synthesis of Biaryl Sulfonyl Fluorides.

Chinthakindi PK, Kruger HG, Govender T, Naicker T, Arvidsson PI

J. Org. Chem. 81 (6) 2618-2623 [2016-03-18; online 2016-02-24]

Drug Discovery and Development (DDD) [Collaborative]

Kinetically Selective Inhibitors of Human Carbonic Anhydrase Isozymes I, II, VII, IX, XII, and XIII.

Talibov VO, Linkuvienė V, Matulis D, Danielson UH

J. Med. Chem. 59 (5) 2083-2093 [2016-03-10; online 2016-01-26]

Drug Discovery and Development (DDD) [Collaborative]

Rapid and straightforward transesterification of sulfonyl carbamates

Isaksson R, Kumpiņa I, Larhed M, Wannberg J

Tetrahedron Letters 57 (13) 1476-1478 [2016-03-00; online 2016-03-00]

Drug Discovery and Development (DDD) [Collaborative]

An Efficient Protecting-Group-Free Synthesis of Vinylic Sulfoximines via Horner–Wadsworth–Emmons Reaction

Naicker T, Arvidsson P, Chinthakindi P, ..., Govender T, Kruger H

Synlett 27 (09) 1423-1427 [2016-02-24; online 2016-02-24]

Drug Discovery and Development (DDD) [Collaborative]

Microwave Promoted Transcarbamylation Reaction of Sulfonylcarbamates under Continuous-Flow Conditions

Kumpiņa I, Isaksson R, Sävmarker J, Wannberg J, Larhed M

Org. Process Res. Dev. 20 (2) 440-445 [2016-02-19; online 2016-01-05]

Drug Discovery and Development (DDD) [Collaborative]

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Collaborative] Protein Science Facility (PSF) [Service]

Stereoselective synthesis towards unnatural proline based amino acids

S.Makhathini S, Das SK, Singh T, ..., Govender T, Naicker T

ARKIVOC 2016 (3) 134-144 [2016-02-07; online 2016-02-07]

Drug Discovery and Development (DDD) [Collaborative]

Ex Vivo Assessment of Drug Activity in Patient Tumor Cells as a Basis for Tailored Cancer Therapy.

Blom K, Nygren P, Alvarsson J, Larsson R, Andersson CR

J Lab Autom 21 (1) 178-187 [2016-02-00; online 2015-08-05]

Organocatalyzed Mannich reactions on minocycline: Towards novel tetracycline antibiotics

CHIWUNZE TE, Azumah R, Ramtahal M, ..., Govender T, Naicker T

S.Afr.j.chem. 69 (-) - [2016-00-00; online 2016-00-00]

Drug Discovery and Development (DDD) [Collaborative]

Year 2015

Positive Modulation of the Glycine Receptor by Means of Glycine Receptor-Binding Aptamers.

Shalaly ND, Aneiros E, Blank M, ..., Andersson CV, Sandberg K

J Biomol Screen 20 (9) 1112-1123 [2015-10-00; online 2015-06-12]

Drug Discovery and Development (DDD) [Collaborative]

Towards a stereoselective synthesis of α,α-disubstituted proline analogues

Das SK, Bhatt N, Mujahid M, ..., Naicker T, Govender T

Tetrahedron Letters 56 (37) 5172-5174 [2015-09-00; online 2015-09-00]

Drug Discovery and Development (DDD) [Collaborative]

Synthesis of enantiopure angiotensin II type 2 receptor [AT2R] antagonist EMA401

Wakchaure PB, Bremberg U, Wannberg J, Larhed M

Tetrahedron 71 (38) 6881-6887 [2015-09-00; online 2015-09-00]

Three-Dimensional Cell Culture-Based Screening Identifies the Anthelmintic Drug Nitazoxanide as a Candidate for Treatment of Colorectal Cancer.

Senkowski W, Zhang X, Olofsson MH, ..., Larsson R, Fryknäs M

Mol Cancer Ther 14 (6) 1504-1516 [2015-06-00; online 2015-04-24]

NOTA: a potent metallo-β-lactamase inhibitor.

Somboro AM, Tiwari D, Bester LA, ..., Naicker T, Essack SY

J. Antimicrob. Chemother. 70 (5) 1594-1596 [2015-05-00; online 2015-01-06]

Drug Discovery and Development (DDD) [Collaborative]

Cu(OAc)2-Catalysed Oxidative Dual C-H/N-H Activation of Terminal Alkynes andN-Deprotected Sulfonimidamides: An Easy Access toN-Alkynylated Sulfonimidamides

Nandi GC, Kota SR, Naicker T, ..., Kruger HG, Arvidsson PI

Eur. J. Org. Chem. 2015 (13) 2861-2867 [2015-05-00; online 2015-03-17]

Drug Discovery and Development (DDD) [Technology development]

Detection of cell aggregation and altered cell viability by automated label-free video microscopy: a promising alternative to endpoint viability assays in high-throughput screening.

Aftab O, Fryknäs M, Hammerling U, Larsson R, Gustafsson MG

J Biomol Screen 20 (3) 372-381 [2015-03-00; online 2014-12-17]

Synthesis of Vinyl- and Aryl-Acyl Sulfonimidamides Through Pd-Catalyzed Carbonylation Using Mo(CO)6as ex situ CO Source

Wakchaure PB, Borhade SR, Sandström A, Arvidsson PI

Eur. J. Org. Chem. 2015 (1) 213-219 [2015-01-00; online 2014-11-19]

Drug Discovery and Development (DDD) [Technology development]

Combining an amyloid-beta (Aβ) cleaving enzyme inhibitor with a γ-secretase modulator results in an additive reduction of Aβ production.

Strömberg K, Eketjäll S, Georgievska B, ..., Cowburn RF, Dabrowski M

FEBS J. 282 (1) 65-73 [2015-01-00; online 2014-11-07]

Drug Discovery and Development (DDD) [Collaborative]

Applied Enantioselective Aminocatalysis: α-Heteroatom Functionalization Reactions on the Carbapenem (β-Lactam Antibiotic) Core

Cele ZED, Arvidsson PI, Kruger HG, Govender T, Naicker T

Eur. J. Org. Chem. 2015 (3) 638-646 [2015-01-00; online 2014-12-11]

Drug Discovery and Development (DDD) [Collaborative]

The effect of N-methylation of amino acids (Ac-X-OMe) on solubility and conformation: a DFT study

Md. Abdur Rauf S, Arvidsson PI, Albericio F, ..., Kruger HG, Honarparvar B

Org. Biomol. Chem. 13 (39) 9993-10006 [2015-00-00; online 2015-00-00]

Drug Discovery and Development (DDD) [Collaborative]

Pd-catalyzed C–N coupling of vinylbromides and sulfonimidamides: a facile synthesis of N′-vinylsulfonimidamides

Nandi GC, Kota SR, Wakchaure PB, ..., Naicker T, Arvidsson PI

RSC Adv. 5 (76) 62084-62090 [2015-00-00; online 2015-00-00]

Drug Discovery and Development (DDD) [Technology development]

Year 2014

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Collaborative]

Cu(OAc)2 promoted Chan–Evans–Lam C–N cross coupling reactions on the N- and N′-nitrogen atoms of sulfonimidamides with aryl boronic acids

Nandi GC, Kota SR, Govender T, Kruger HG, Arvidsson PI

Tetrahedron 70 (35) 5428-5433 [2014-09-00; online 2014-09-00]

Drug Discovery and Development (DDD) [Technology development]

l-Proline organocatalyzed Michael synthesis of monobactam and carbapenem β-lactam cores

Khanyase S, Naicker T, Maguire GEM, ..., Arvidsson PI, Govender T

Tetrahedron: Asymmetry 25 (13-14) 969-973 [2014-07-00; online 2014-07-00]

Drug Discovery and Development (DDD) [Collaborative]

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 (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Collaborative] Protein Science Facility (PSF)

Organocatalytic Mannich Reactions on a Carbapenem Core - Synthesis of Mannich Bases and Bicyclic Diazanonanes

Cele ZED, Pawar SA, Naicker T, ..., Kruger HG, Govender T

Eur. J. Org. Chem. 2014 (11) 2253-2260 [2014-04-00; online 2014-02-06]

Drug Discovery and Development (DDD) [Collaborative]

Proline N-oxides: modulators of the 3D conformation of linear peptides through “NO-turns”

Farahani MD, Honarparvar B, Albericio F, ..., Arvidsson PI, Kruger HG

Org. Biomol. Chem. 12 (25) 4479 [2014-00-00; online 2014-00-00]

Drug Discovery and Development (DDD) [Collaborative]

Year 2013

Comparative drug pair screening across multiple glioblastoma cell lines reveals novel drug-drug interactions.

Schmidt L, Kling T, Monsefi N, ..., Gerlee P, Nelander S

Neuro-oncology 15 (11) 1469-1478 [2013-11-00; online 2013-10-06]

Drug Discovery and Development (DDD) [Collaborative]