Burke JR - Search Results

1

Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.

Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. Among authors: burke jr. J Med Chem. 2016 Oct 13;59(19):9173-9200. doi: 10.1021/acs.jmedchem.6b01088. Epub 2016 Sep 19. J Med Chem. 2016. PMID: 27583770

2

BMS-345541 is a highly selective inhibitor of I kappa B kinase that binds at an allosteric site of the enzyme and blocks NF-kappa B-dependent transcription in mice.

Burke JR, Pattoli MA, Gregor KR, Brassil PJ, MacMaster JF, McIntyre KW, Yang X, Iotzova VS, Clarke W, Strnad J, Qiu Y, Zusi FC. Burke JR, et al. J Biol Chem. 2003 Jan 17;278(3):1450-6. doi: 10.1074/jbc.M209677200. Epub 2002 Oct 25. J Biol Chem. 2003. PMID: 12403772 Free article.

3

A highly selective inhibitor of I kappa B kinase, BMS-345541, blocks both joint inflammation and destruction in collagen-induced arthritis in mice.

McIntyre KW, Shuster DJ, Gillooly KM, Dambach DM, Pattoli MA, Lu P, Zhou XD, Qiu Y, Zusi FC, Burke JR. McIntyre KW, et al. Among authors: burke jr. Arthritis Rheum. 2003 Sep;48(9):2652-9. doi: 10.1002/art.11131. Arthritis Rheum. 2003. PMID: 13130486 Free article.

4

A highly selective inhibitor of IkappaB kinase, BMS-345541, augments graft survival mediated by suboptimal immunosuppression in a murine model of cardiac graft rejection.

Townsend RM, Postelnek J, Susulic V, McIntyre KW, Shuster DJ, Qiu Y, Zusi FC, Burke JR. Townsend RM, et al. Among authors: burke jr. Transplantation. 2004 Apr 15;77(7):1090-4. doi: 10.1097/01.tp.0000118407.05205.05. Transplantation. 2004. PMID: 15087776

5

Collagen and aggrecan degradation is blocked in interleukin-1-treated cartilage explants by an inhibitor of IkappaB kinase through suppression of metalloproteinase expression.

Pattoli MA, MacMaster JF, Gregor KR, Burke JR. Pattoli MA, et al. Among authors: burke jr. J Pharmacol Exp Ther. 2005 Oct;315(1):382-8. doi: 10.1124/jpet.105.087569. Epub 2005 Jul 11. J Pharmacol Exp Ther. 2005. PMID: 16009742

6

NEMO binding domain of IKK-2 encompasses amino acids 735-745.

Strnad J, McDonnell PA, Riexinger DJ, Mapelli C, Cheng L, Gray H, Ryseck RP, Burke JR. Strnad J, et al. Among authors: burke jr. J Mol Recognit. 2006 May-Jun;19(3):227-33. doi: 10.1002/jmr.766. J Mol Recognit. 2006. PMID: 16583354

7

Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors.

Beaulieu F, Ouellet C, Ruediger EH, Belema M, Qiu Y, Yang X, Banville J, Burke JR, Gregor KR, MacMaster JF, Martel A, McIntyre KW, Pattoli MA, Zusi FC, Vyas D. Beaulieu F, et al. Among authors: burke jr. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1233-7. doi: 10.1016/j.bmcl.2006.12.017. Epub 2006 Dec 9. Bioorg Med Chem Lett. 2007. PMID: 17197177

8

Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.

Belema M, Bunker A, Nguyen VN, Beaulieu F, Ouellet C, Qiu Y, Zhang Y, Martel A, Burke JR, McIntyre KW, Pattoli MA, Daloisio C, Gillooly KM, Clarke WJ, Brassil PJ, Zusi FC, Vyas DM. Belema M, et al. Among authors: burke jr. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4284-9. doi: 10.1016/j.bmcl.2007.05.031. Epub 2007 May 16. Bioorg Med Chem Lett. 2007. PMID: 17540562

9

Novel tricyclic inhibitors of IkappaB kinase.

Kempson J, Spergel SH, Guo J, Quesnelle C, Gill P, Belanger D, Dyckman AJ, Li T, Watterson SH, Langevine CM, Das J, Moquin RV, Furch JA, Marinier A, Dodier M, Martel A, Nirschl D, Van Kirk K, Burke JR, Pattoli MA, Gillooly K, McIntyre KW, Chen L, Yang Z, Marathe PH, Wang-Iverson D, Dodd JH, McKinnon M, Barrish JC, Pitts WJ. Kempson J, et al. Among authors: burke jr. J Med Chem. 2009 Apr 9;52(7):1994-2005. doi: 10.1021/jm8015816. J Med Chem. 2009. PMID: 19267461

10

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.

Kempson J, Guo J, Das J, Moquin RV, Spergel SH, Watterson SH, Langevine CM, Dyckman AJ, Pattoli M, Burke JR, Yang X, Gillooly KM, McIntyre KW, Chen L, Dodd JH, McKinnon M, Barrish JC, Pitts WJ. Kempson J, et al. Among authors: burke jr. Bioorg Med Chem Lett. 2009 May 15;19(10):2646-9. doi: 10.1016/j.bmcl.2009.03.159. Epub 2009 Apr 5. Bioorg Med Chem Lett. 2009. PMID: 19376699

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