Drug Discovery and Development (DDD)

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Publications

2020 (159)

2019 (744)

2018 (669)

2017 (698)

2016 (671)

2015 (431)

2014 (376)

2013 (320)

2012 (243)

2011 (163)

2010 (139)

All (4613)


Facilities

Journals

SciLifeLab National platform since 2013. Includes facilities ADME of Therapeautics, Biochemical and cellular screening, Biophysical Screening and Characterization, Human Antibody Therapeutics, In Vitro and Systems Pharmacology, Medicinal Chemistry – Hit2lead, Medicinal Chemistry – Lead Identification, Protein Expression and Characterization.

97 publications

Year 2020

DOI Crossref
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 (-) 3915-3934 [2020-04-08; online 2020-04-08]
Chemical Biology Consortium Sweden (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Collaborative]

Year 2019

DOI Crossref
Estimating Detection Limits of Potentiometric DNA Sensors Using Surface Plasmon Resonance Analyses
Xu X, Makaraviciute A, Abdurakhmanov E, ..., Nyholm L, Zhang Z
ACS Sens. - (-) - [2019-12-23; online 2019-12-23]
Drug Discovery and Development (DDD) [Technology development]
DOI Crossref
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) - [2019-12-00; online 2019-10-28]
Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Service]
DOI Crossref
A Cell-Free Approach Based on Phospholipid Characterization for Determination of the Cell Specific Unbound Drug Fraction (fu,cell)
Treyer A, Walday S, Boriss H, Matsson P, Artursson P
Pharm Res 36 (12) - [2019-12-00; online 2019-11-07]
Drug Discovery and Development (DDD) [Technology development]
DOI Crossref
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) - [2019-12-00; online 2019-04-10]
Drug Discovery and Development (DDD) [Technology development]
DOI Crossref
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 2019-10-25]
Drug Discovery and Development (DDD) [Technology development]
DOI Crossref
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]
PubMed DOI Crossref
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 (-) - [2019-05-17; online 2019-05-17]
Drug Discovery and Development (DDD) [Collaborative] Plasma Profiling [Collaborative]
DOI Crossref
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]
DOI Crossref
A Series of Analogues to the AT2 R 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]
DOI Crossref
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 [2019-00-00; online 2019-00-00]
Drug Discovery and Development (DDD) [Service]

Year 2018

PubMed DOI Crossref
Targeting PFKFB3 radiosensitizes cancer cells and suppresses homologous recombination
Gustafsson NMS, Färnegårdh K, Bonagas N, ..., Olin T, Helleday T
PDB
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]
PubMed DOI Crossref
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
PDB GEO
Nat Commun 9 (1) - [2018-12-00; 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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
Targeted NUDT5 inhibitors block hormone signaling in breast cancer cells
Page BDG, Valerie NCK, Wright RHG, ..., Beato M, Helleday T
PDB PDB
Nat Commun 9 (1) - [2018-12-00; online 2018-01-17]
Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Service] Protein Science Facility (PSF) [Service]
PubMed DOI Crossref
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 2018-11-15]
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]
PubMed DOI Crossref
Targeted Analysis of Serum Proteins Encoded at Known Inflammatory Bowel Disease Risk Loci
Drobin K, Assadi G, Hong MG, ..., D’Amato M, Halfvarson J
- - (-) - [2018-10-24; online 2018-10-24]
Bioinformatics Compute and Storage [Service] Drug Discovery and Development (DDD) [Collaborative] Plasma Profiling [Collaborative]
DOI Crossref
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]
DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
Drug Discovery and Development (DDD) [Service]
DOI Crossref
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 2018-02-21]
Drug Discovery and Development (DDD) [Service]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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
pmc
PLoS ONE 13 (2) e0189116 [2018-02-13; online 2018-02-13]
Drug Discovery and Development (DDD) [Technology development]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
DOI Crossref
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]
DOI Crossref
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

PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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 - (-) 1-7 [2017-10-13; online 2017-10-13]
Drug Discovery and Development (DDD) [Collaborative]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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
New Biotechnology - (-) - [2017-08-00; online 2017-08-00]
Drug Discovery and Development (DDD) [Technology development]
DOI Crossref
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 - (-) - [2017-08-00; online 2017-08-00]
Drug Discovery and Development (DDD) [Collaborative]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
DOI Crossref
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]
DOI Crossref
On the bridge over the translational valley of death: interview with Per I Arvidsson
Arvidsson PI
Future Science OA 3 (2) FSO183 [2017-05-00; online 2017-05-00]
Drug Discovery and Development (DDD) [Technology development]
PubMed DOI Crossref
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]
Drug Discovery and Development (DDD) [Service]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
Drug Discovery and Development (DDD) [Service]
PubMed DOI Crossref
Intracellular drug bioavailability: a new predictor of system dependent drug disposition.
Mateus A, Treyer A, Wegler C, ..., Matsson P, Artursson P
pmc
Sci Rep 7 (-) 43047 [2017-02-22; online 2017-02-22]
Drug Discovery and Development (DDD) [Service]
PubMed DOI Crossref
Crystal Structure of the Emerging Cancer Target MTHFD2 in Complex with a Substrate-Based Inhibitor.
Gustafsson R, Jemth A, Gustafsson NMS, ..., Helleday T, Stenmark P
Cancer Res. 77 (4) 937-948 [2017-02-15; online 2016-12-03]
Drug Discovery and Development (DDD) [Collaborative]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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 [2017-00-00; online 2017-00-00]
Drug Discovery and Development (DDD) [Collaborative]

Year 2016

PubMed DOI Crossref
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]
PubMed DOI Crossref
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) [Technology development] Tissue Profiling [Service]
PubMed DOI Crossref
Case-specific potentiation of glioblastoma drugs by pterostilbene.
Schmidt L, Baskaran S, Johansson P, ..., Krona C, Nelander S
pmc
Oncotarget 7 (45) 73200-73215 [2016-11-08; online 2016-10-01]
Drug Discovery and Development (DDD) [Collaborative]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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 2016-05-12]
Drug Discovery and Development (DDD) [Collaborative]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
DOI Crossref
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]
PubMed DOI Crossref
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]
PubMed DOI Crossref
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]
DOI Crossref
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]
DOI Crossref
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]
DOI Crossref
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 2016-02-19]
Drug Discovery and Development (DDD) [Collaborative]
PubMed DOI Crossref
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 2016-02-11]
Chemical Biology Consortium Sweden (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Collaborative] Protein Science Facility (PSF) [Service]
DOI Crossref
Stereoselective synthesis towards unnatural proline based amino acids
Makhathini SS, Das SK, Singh T, ..., Govender T, Naicker T
ARKIVOC 2016 (3) 134 [2016-02-07; online 2016-02-07]
Drug Discovery and Development (DDD) [Collaborative]
DOI Crossref
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

DOI Crossref
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 2015-10-00]
Drug Discovery and Development (DDD) [Collaborative]
DOI Crossref
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]
Drug Discovery and Development (DDD)
DOI Crossref
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]
DOI Crossref
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]
DOI Crossref
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]
DOI Crossref
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]
DOI Crossref
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]
DOI Crossref
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]
DOI Crossref
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]
PubMed DOI Crossref
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]

Year 2014

PubMed DOI Crossref
Inhibition of Insulin-Regulated Aminopeptidase (IRAP) by Arylsulfonamides.
Borhade SR, Rosenström U, Sävmarker J, ..., Larhed M, Hallberg M
pmc
ChemistryOpen 3 (6) 256-263 [2014-12-00; online 2014-11-21]
Chemical Biology Consortium Sweden (CBCS) [Collaborative] Drug Discovery and Development (DDD) [Collaborative]
DOI Crossref
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]
DOI Crossref
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]
PubMed DOI Crossref
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)
DOI Crossref
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]
PubMed DOI Crossref
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

PubMed DOI Crossref
Comparative drug pair screening across multiple glioblastoma cell lines reveals novel drug-drug interactions.
Schmidt L, Kling T, Monsefi N, ..., Gerlee P, Nelander S
pmc
Neuro-oncology 15 (11) 1469-1478 [2013-11-00; online 2013-10-06]
Drug Discovery and Development (DDD) [Collaborative]
PubMed DOI Crossref
Retinoic acid receptor alpha is associated with tamoxifen resistance in breast cancer.
Johansson HJ, Sanchez BC, Mundt F, ..., Linderholm BK, Lehtiö J
pmc
Nat Commun 4 (-) 2175 [2013-07-23; online 2013-07-23]
Drug Discovery and Development (DDD) [Collaborative]
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