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Page 1
Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors.
Liu H, Kuhn C, Feru F, Jacques SL, Deshmukh GD, Ye P, Rennie GR, Johnson T, Kazmirski S, Low S, Coli R, Ding YH, Cheng AC, Tecle H, English JM, Stanton R, Wu JC. Liu H, et al. Among authors: tecle h. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4885-91. doi: 10.1016/j.bmcl.2010.06.073. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20620059
The design, synthesis and potential utility of fluorescence probes that target DFG-out conformation of p38alpha for high throughput screening binding assay.
Tecle H, Feru F, Liu H, Kuhn C, Rennie G, Morris M, Shao J, Cheng AC, Gikunju D, Miret J, Coli R, Xi SH, Clugston SL, Low S, Kazmirski S, Ding YH, Cao Q, Johnson TL, Deshmukh GD, DiNitto JP, Wu JC, English JM. Tecle H, et al. Chem Biol Drug Des. 2009 Dec;74(6):547-59. doi: 10.1111/j.1747-0285.2009.00884.x. Epub 2009 Oct 20. Chem Biol Drug Des. 2009. PMID: 19843080
2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase).
Warmus JS, Flamme C, Zhang LY, Barrett S, Bridges A, Chen H, Gowan R, Kaufman M, Sebolt-Leopold J, Leopold W, Merriman R, Ohren J, Pavlovsky A, Przybranowski S, Tecle H, Valik H, Whitehead C, Zhang E. Warmus JS, et al. Among authors: tecle h. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6171-4. doi: 10.1016/j.bmcl.2008.10.015. Epub 2008 Oct 7. Bioorg Med Chem Lett. 2008. PMID: 18951019
N-(6,7-dichloro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)-N-alkylsulfonamides as peripherally restricted N-methyl-D-aspartate receptor antagonists for the treatment of pain.
Deur C, Agrawal AK, Baum H, Booth J, Bove S, Brieland J, Bunker A, Connolly C, Cornicelli J, Dumin J, Finzel B, Gan X, Guppy S, Kamilar G, Kilgore K, Lee P, Loi CM, Lou Z, Morris M, Philippe L, Przybranowski S, Riley F, Samas B, Sanchez B, Tecle H, Wang Z, Welch K, Wilson M, Yates K. Deur C, et al. Among authors: tecle h. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4599-603. doi: 10.1016/j.bmcl.2007.05.083. Epub 2007 May 31. Bioorg Med Chem Lett. 2007. PMID: 17562362
The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
Barrett SD, Bridges AJ, Dudley DT, Saltiel AR, Fergus JH, Flamme CM, Delaney AM, Kaufman M, LePage S, Leopold WR, Przybranowski SA, Sebolt-Leopold J, Van Becelaere K, Doherty AM, Kennedy RM, Marston D, Howard WA Jr, Smith Y, Warmus JS, Tecle H. Barrett SD, et al. Among authors: tecle h. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. doi: 10.1016/j.bmcl.2008.10.054. Epub 2008 Oct 15. Bioorg Med Chem Lett. 2008. PMID: 18952427
Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.
Smaill JB, Gonzales AJ, Spicer JA, Lee H, Reed JE, Sexton K, Althaus IW, Zhu T, Black SL, Blaser A, Denny WA, Ellis PA, Fakhoury S, Harvey PJ, Hook K, McCarthy FO, Palmer BD, Rivault F, Schlosser K, Ellis T, Thompson AM, Trachet E, Winters RT, Tecle H, Bridges A. Smaill JB, et al. Among authors: tecle h. J Med Chem. 2016 Sep 8;59(17):8103-24. doi: 10.1021/acs.jmedchem.6b00883. Epub 2016 Aug 22. J Med Chem. 2016. PMID: 27491023
4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase.
Spicer JA, Rewcastle GW, Kaufman MD, Black SL, Plummer MS, Denny WA, Quin J 3rd, Shahripour AB, Barrett SD, Whitehead CE, Milbank JB, Ohren JF, Gowan RC, Omer C, Camp HS, Esmaeil N, Moore K, Sebolt-Leopold JS, Pryzbranowski S, Merriman RL, Ortwine DF, Warmus JS, Flamme CM, Pavlovsky AG, Tecle H. Spicer JA, et al. Among authors: tecle h. J Med Chem. 2007 Oct 18;50(21):5090-102. doi: 10.1021/jm0704548. Epub 2007 Sep 19. J Med Chem. 2007. PMID: 17880056
Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition.
Ohren JF, Chen H, Pavlovsky A, Whitehead C, Zhang E, Kuffa P, Yan C, McConnell P, Spessard C, Banotai C, Mueller WT, Delaney A, Omer C, Sebolt-Leopold J, Dudley DT, Leung IK, Flamme C, Warmus J, Kaufman M, Barrett S, Tecle H, Hasemann CA. Ohren JF, et al. Among authors: tecle h. Nat Struct Mol Biol. 2004 Dec;11(12):1192-7. doi: 10.1038/nsmb859. Epub 2004 Nov 14. Nat Struct Mol Biol. 2004. PMID: 15543157
24 results