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Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS. Wrobleski ST, et al. Among authors: aranibar n. J Med Chem. 2019 Oct 24;62(20):8973-8995. doi: 10.1021/acs.jmedchem.9b00444. Epub 2019 Jul 18. J Med Chem. 2019. PMID: 31318208
Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).
Watterson SH, Xiao Z, Dodd DS, Tortolani DR, Vaccaro W, Potin D, Launay M, Stetsko DK, Skala S, Davis PM, Lee D, Yang X, McIntyre KW, Balimane P, Patel K, Yang Z, Marathe P, Kadiyala P, Tebben AJ, Sheriff S, Chang CY, Ziemba T, Zhang H, Chen BC, DelMonte AJ, Aranibar N, McKinnon M, Barrish JC, Suchard SJ, Murali Dhar TG. Watterson SH, et al. Among authors: aranibar n. J Med Chem. 2010 May 13;53(9):3814-30. doi: 10.1021/jm100348u. J Med Chem. 2010. PMID: 20405922
Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.
Moslin R, Gardner D, Santella J, Zhang Y, Duncia JV, Liu C, Lin J, Tokarski JS, Strnad J, Pedicord D, Chen J, Blat Y, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Sack JS, Muckelbauer JK, Chang C, Tredup J, Xie D, Aranibar N, Burke JR, Carter PH, Weinstein DS. Moslin R, et al. Among authors: aranibar n. Medchemcomm. 2016 Dec 15;8(4):700-712. doi: 10.1039/c6md00560h. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108788 Free PMC article.
Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.
Liu C, Lin J, Moslin R, Tokarski JS, Muckelbauer J, Chang C, Tredup J, Xie D, Park H, Li P, Wu DR, Strnad J, Zupa-Fernandez A, Cheng L, Chaudhry C, Chen J, Chen C, Sun H, Elzinga P, D'arienzo C, Gillooly K, Taylor TL, McIntyre KW, Salter-Cid L, Lombardo LJ, Carter PH, Aranibar N, Burke JR, Weinstein DS. Liu C, et al. Among authors: aranibar n. ACS Med Chem Lett. 2019 Feb 21;10(3):383-388. doi: 10.1021/acsmedchemlett.9b00035. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891145 Free PMC article.
Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).
Moslin R, Zhang Y, Wrobleski ST, Lin S, Mertzman M, Spergel S, Tokarski JS, Strnad J, Gillooly K, McIntyre KW, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Heimrich E, Yang X, Muckelbauer JK, Chang C, Tredup J, Mulligan D, Xie D, Aranibar N, Chiney M, Burke JR, Lombardo L, Carter PH, Weinstein DS. Moslin R, et al. Among authors: aranibar n. J Med Chem. 2019 Oct 24;62(20):8953-8972. doi: 10.1021/acs.jmedchem.9b00443. Epub 2019 Jul 17. J Med Chem. 2019. PMID: 31314518
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Xiao Z, Yang MG, Liu C, Sherwood T, Gilmore JL, Lin J, Li P, Wu DR, Tokarski J, Li S, Cheng L, Xie C, Fan J, Dierks E, Strnad J, Cvijic ME, Khan J, Ruzanov M, Galella M, Khandelwal P, Dyckman AJ, Mathur A, Lombardo LJ, Macor JE, Carter PH, Aranibar N, Burke JR, Weinstein DS. Xiao Z, et al. Among authors: aranibar n. Bioorg Med Chem Lett. 2023 Jul 15;91:129373. doi: 10.1016/j.bmcl.2023.129373. Epub 2023 Jun 12. Bioorg Med Chem Lett. 2023. PMID: 37315697
Urinary metabolites of 2-bromoethanamine identified by stable isotope labelling: evidence for carbamoylation and glutathione conjugation.
Shipkova P, Vassallo JD, Aranibar N, Hnatyshyn S, Zhang H, Clayton TA, Cantor GH, Sanders M, Coen M, Lindon JC, Holmes E, Nicholson JK, Lehman-McKeeman L. Shipkova P, et al. Among authors: aranibar n. Xenobiotica. 2011 Feb;41(2):144-54. doi: 10.3109/00498254.2010.529179. Epub 2010 Nov 2. Xenobiotica. 2011. PMID: 21043805
31 results