Drug Discovery and Development (DDD)

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.

123 publications

Year 2020

Mebendazole is unique among tubulin-active drugs in activating the MEK-ERK pathway.
Andersson CR, Selvin T, Blom K, ..., Nygren P, Larsson R
pii: 10.1038/s41598-020-68986-0 pmc: PMC7403428
Sci Rep 10 (1) 13124 [2020-08-04; online 2020-08-04]
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
pii: S2211-1247(20)30878-0
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
pii: 10.1186/s13023-020-01437-1 pmc: PMC7325660
Orphanet J Rare Dis 15 (1) 170 [2020-06-30; online 2020-06-30]
Drug Discovery and Development (DDD)
Comprehensive chemical proteomics for target deconvolution of the redox active drug auranofin.
Saei AA, Gullberg H, Sabatier P, ..., Arnér ESJ, Zubarev RA
pii: S2213-2317(20)30243-3 pmc: PMC7082630
Redox Biol 32 (-) 101491 [2020-05-00; online 2020-03-03]
Drug Discovery and Development (DDD)

Year 2019

Mebendazole-induced M1 polarisation of THP-1 macrophages may involve DYRK1B inhibition.
Blom K, Rubin J, Berglund M, ..., Nygren P, Larsson R
pii: 10.1186/s13104-019-4273-5 pmc: PMC6477744
BMC Res Notes 12 (1) 234 [2019-04-22; online 2019-04-22]
Drug Discovery and Development (DDD) [Service]

Year 2018

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
OSF: https://osf.io/sreqf/?view_only=bd0c5cd611be481984ef164d5d15df3d
PLoS ONE 13 (4) e0195956 [2018-04-23; online 2018-04-23]
Drug Discovery and Development (DDD) [Service]
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
pii: PONE-D-17-23519 pmc: PMC5810979 PeptideAtlas: PASS00852
PLoS ONE 13 (2) e0189116 [2018-02-13; online 2018-02-13]
Drug Discovery and Development (DDD) [Technology development]
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]

Year 2017

Targeting tumor cells based on Phosphodiesterase 3A expression.
Nazir M, Senkowski W, Nyberg F, ..., Larsson R, Fryknäs M
pii: S0014-4827(17)30580-3
Exp. Cell Res. 361 (2) 308-315 [2017-12-15; online 2017-10-26]
Drug Discovery and Development (DDD) [Service]
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
pii: S0145-2126(17)30565-9
Leuk Res 63 (-) 41-46 [2017-12-00; online 2017-10-28]
Drug Discovery and Development (DDD) [Service]
Glioblastoma Cell Malignancy and Drug Sensitivity Are Affected by the Cell of Origin.
Jiang Y, Marinescu VD, Xie Y, ..., Nelander S, Uhrbom L
pii: S2211-1247(17)30564-8
Cell Rep 19 (5) 1080-1081 [2017-05-02; online 2017-05-04]
Drug Discovery and Development (DDD) [Service]
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
pii: nature22083
Nature 544 (7651) 508 [2017-04-26; online 2017-04-28]
Drug Discovery and Development (DDD) [Service]
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]
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
pii: 0008-5472.CAN-16-1476
Cancer Res. 77 (4) 937-948 [2017-02-15; online 2016-12-03]
Drug Discovery and Development (DDD) [Collaborative]

Year 2016

Iron chelators target both proliferating and quiescent cancer cells.
Fryknäs M, Zhang X, Bremberg U, ..., Linder S, Larsson R
pii: srep38343 pmc: PMC5141479
Sci Rep 6 (-) 38343 [2016-12-07; online 2016-12-07]
Drug Discovery and Development (DDD) [Service]
Case-specific potentiation of glioblastoma drugs by pterostilbene.
Schmidt L, Baskaran S, Johansson P, ..., Krona C, Nelander S
pii: 12298 pmc: PMC5341973
Oncotarget 7 (45) 73200-73215 [2016-11-08; online 2016-10-01]
Drug Discovery and Development (DDD) [Collaborative]
Biophysics in drug discovery: impact, challenges and opportunities.
Renaud JP, Chung CW, Danielson UH, ..., Hubbard RE, Nar H
pii: nrd.2016.123
Nat Rev Drug Discov 15 (10) 679-698 [2016-10-00; online 2016-08-16]
Drug Discovery and Development (DDD) [Technology development]
Repeated LPS Injection Induces Distinct Changes in the Kynurenine Pathway in Mice.
Larsson MK, Faka A, Bhat M, ..., Schwieler L, Erhardt S
pii: 10.1007/s11064-016-1939-4
Neurochem. Res. 41 (9) 2243-2255 [2016-09-00; online 2016-05-12]
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
pii: 10.1007/s10735-016-9685-0
J. Mol. Histol. 47 (4) 429-435 [2016-08-00; online 2016-06-22]
Drug Discovery and Development (DDD) [Collaborative]
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]
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]
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
pii: 2211068215598117
J Lab Autom 21 (1) 178-187 [2016-02-00; online 2015-08-05]
Drug Discovery and Development (DDD) [Service]

Year 2015

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)
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]
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

Year 2013

Retinoic acid receptor alpha is associated with tamoxifen resistance in breast cancer.
Johansson HJ, Sanchez BC, Mundt F, ..., Linderholm BK, Lehtiö J
pii: ncomms3175 pmc: PMC3759040
Nat Commun 4 (-) 2175 [2013-07-23; online 2013-07-23]
Drug Discovery and Development (DDD) [Collaborative]