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Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.
Chen P, Doweyko AM, Norris D, Gu HH, Spergel SH, Das J, Moquin RV, Lin J, Wityak J, Iwanowicz EJ, McIntyre KW, Shuster DJ, Behnia K, Chong S, de Fex H, Pang S, Pitt S, Shen DR, Thrall S, Stanley P, Kocy OR, Witmer MR, Kanner SB, Schieven GL, Barrish JC. Chen P, et al. Among authors: witmer mr. J Med Chem. 2004 Aug 26;47(18):4517-29. doi: 10.1021/jm030217e. J Med Chem. 2004. PMID: 15317463
Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Gentles RG, Ding M, Bender JA, Bergstrom CP, Grant-Young K, Hewawasam P, Hudyma T, Martin S, Nickel A, Regueiro-Ren A, Tu Y, Yang Z, Yeung KS, Zheng X, Chao S, Sun JH, Beno BR, Camac DM, Chang CH, Gao M, Morin PE, Sheriff S, Tredup J, Wan J, Witmer MR, Xie D, Hanumegowda U, Knipe J, Mosure K, Santone KS, Parker DD, Zhuo X, Lemm J, Liu M, Pelosi L, Rigat K, Voss S, Wang Y, Wang YK, Colonno RJ, Gao M, Roberts SB, Gao Q, Ng A, Meanwell NA, Kadow JF. Gentles RG, et al. Among authors: witmer mr. J Med Chem. 2014 Mar 13;57(5):1855-79. doi: 10.1021/jm4016894. Epub 2014 Jan 7. J Med Chem. 2014. PMID: 24397558
Pharmacologic profile of the Adnectin BMS-962476, a small protein biologic alternative to PCSK9 antibodies for low-density lipoprotein lowering.
Mitchell T, Chao G, Sitkoff D, Lo F, Monshizadegan H, Meyers D, Low S, Russo K, DiBella R, Denhez F, Gao M, Myers J, Duke G, Witmer M, Miao B, Ho SP, Khan J, Parker RA. Mitchell T, et al. Among authors: witmer m. J Pharmacol Exp Ther. 2014 Aug;350(2):412-24. doi: 10.1124/jpet.114.214221. Epub 2014 Jun 10. J Pharmacol Exp Ther. 2014. PMID: 24917546
Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain.
Tokarski JS, Zupa-Fernandez A, Tredup JA, Pike K, Chang C, Xie D, Cheng L, Pedicord D, Muckelbauer J, Johnson SR, Wu S, Edavettal SC, Hong Y, Witmer MR, Elkin LL, Blat Y, Pitts WJ, Weinstein DS, Burke JR. Tokarski JS, et al. J Biol Chem. 2015 Apr 24;290(17):11061-74. doi: 10.1074/jbc.M114.619502. Epub 2015 Mar 11. J Biol Chem. 2015. PMID: 25762719 Free PMC article.
Development of a RapidFire mass spectrometry assay and a fluorescence assay for the discovery of kynurenine aminotransferase II inhibitors to treat central nervous system disorders.
Lu H, Kopcho L, Ghosh K, Witmer M, Parker M, Gupta S, Paul M, Krishnamurthy P, Laksmaiah B, Xie D, Tredup J, Zhang L, Abell LM. Lu H, et al. Among authors: witmer m. Anal Biochem. 2016 May 15;501:56-65. doi: 10.1016/j.ab.2016.02.003. Epub 2016 Feb 11. Anal Biochem. 2016. PMID: 26874021
Biotechnology Based Process for Production of a Disulfide-Bridged Peptide.
Goswami A, Goldberg SL, Hanson RL, Johnston RM, Lyngberg OK, Chan Y, Lo E, Chan SH, de Mas N, Ramirez A, Doyle R, Ding W, Gao M, Krystek SR Jr, Wan C, Kim YJ, Calambur D, Witmer M, Bryson JW. Goswami A, et al. Among authors: witmer m. Bioconjug Chem. 2016 May 18;27(5):1276-84. doi: 10.1021/acs.bioconjchem.6b00101. Epub 2016 May 2. Bioconjug Chem. 2016. PMID: 27098672
Exploration of macrocyclic peptide binders to the extracellular CRD domain of human receptor tyrosine kinase-like orphan receptor 1 (ROR1).
Qiao JX, Witmer MR, Lee V, Wang TC, Reid PC, Arioka Y, Farr G, Hill-Drzewi M, Schweizer L, Yamniuk A, Cheng L, Abramczyk B, Corbett M, Calambur D, Szapiel N, Ryseck R, Ponath P, Poss MA, Carter P. Qiao JX, et al. Among authors: witmer mr. Bioorg Med Chem Lett. 2024 Jan 15;98:129589. doi: 10.1016/j.bmcl.2023.129589. Epub 2023 Dec 13. Bioorg Med Chem Lett. 2024. PMID: 38097140
The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.
Wrobleski ST, Lin S, Dhar TG, Dyckman AJ, Li T, Pitt S, Zhang R, Fan Y, Doweyko AM, Tokarski JS, Kish KF, Kiefer SE, Sack JS, Newitt JA, Witmer MR, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K. Wrobleski ST, et al. Among authors: witmer mr. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4120-6. doi: 10.1016/j.bmcl.2013.05.047. Epub 2013 May 23. Bioorg Med Chem Lett. 2013. PMID: 23746475
124 results