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Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans.
Evans EK, Tester R, Aslanian S, Karp R, Sheets M, Labenski MT, Witowski SR, Lounsbury H, Chaturvedi P, Mazdiyasni H, Zhu Z, Nacht M, Freed MI, Petter RC, Dubrovskiy A, Singh J, Westlin WF. Evans EK, et al. Among authors: petter rc. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28. doi: 10.1124/jpet.113.203489. Epub 2013 May 24. J Pharmacol Exp Ther. 2013. PMID: 23709115 Clinical Trial.
Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.
Walter AO, Sjin RT, Haringsma HJ, Ohashi K, Sun J, Lee K, Dubrovskiy A, Labenski M, Zhu Z, Wang Z, Sheets M, St Martin T, Karp R, van Kalken D, Chaturvedi P, Niu D, Nacht M, Petter RC, Westlin W, Lin K, Jaw-Tsai S, Raponi M, Van Dyke T, Etter J, Weaver Z, Pao W, Singh J, Simmons AD, Harding TC, Allen A. Walter AO, et al. Among authors: petter rc. Cancer Discov. 2013 Dec;3(12):1404-15. doi: 10.1158/2159-8290.CD-13-0314. Epub 2013 Sep 24. Cancer Discov. 2013. PMID: 24065731 Free PMC article.
In vitro and in vivo characterization of irreversible mutant-selective EGFR inhibitors that are wild-type sparing.
Tjin Tham Sjin R, Lee K, Walter AO, Dubrovskiy A, Sheets M, Martin TS, Labenski MT, Zhu Z, Tester R, Karp R, Medikonda A, Chaturvedi P, Ren Y, Haringsma H, Etter J, Raponi M, Simmons AD, Harding TC, Niu D, Nacht M, Westlin WF, Petter RC, Allen A, Singh J. Tjin Tham Sjin R, et al. Among authors: petter rc. Mol Cancer Ther. 2014 Jun;13(6):1468-79. doi: 10.1158/1535-7163.MCT-13-0966. Epub 2014 Apr 10. Mol Cancer Ther. 2014. PMID: 24723450
Targeted covalent drugs of the kinase family.
Singh J, Petter RC, Kluge AF. Singh J, et al. Among authors: petter rc. Curr Opin Chem Biol. 2010 Aug;14(4):475-80. doi: 10.1016/j.cbpa.2010.06.168. Epub 2010 Jul 6. Curr Opin Chem Biol. 2010. PMID: 20609616
An assessment of the mechanistic differences between two integrin alpha 4 beta 1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis.
Leone DR, Giza K, Gill A, Dolinski BM, Yang W, Perper S, Scott DM, Lee WC, Cornebise M, Wortham K, Nickerson-Nutter C, Chen LL, LePage D, Spell JC, Whalley ET, Petter RC, Adams SP, Lobb RR, Pepinsky RB. Leone DR, et al. Among authors: petter rc. J Pharmacol Exp Ther. 2003 Jun;305(3):1150-62. doi: 10.1124/jpet.102.047332. Epub 2003 Mar 6. J Pharmacol Exp Ther. 2003. PMID: 12626659
The resurgence of covalent drugs.
Singh J, Petter RC, Baillie TA, Whitty A. Singh J, et al. Among authors: petter rc. Nat Rev Drug Discov. 2011 Apr;10(4):307-17. doi: 10.1038/nrd3410. Nat Rev Drug Discov. 2011. PMID: 21455239 Review.
Design, synthesis, and analysis of a polyethelene glycol-modified (PEGylated) small molecule inhibitor of integrin {alpha}4{beta}1 with improved pharmaceutical properties.
Pepinsky RB, Lee WC, Cornebise M, Gill A, Wortham K, Chen LL, Leone DR, Giza K, Dolinski BM, Perper S, Nickerson-Nutter C, Lepage D, Chakraborty A, Whalley ET, Petter RC, Adams SP, Lobb RR, Scott DM. Pepinsky RB, et al. Among authors: petter rc. J Pharmacol Exp Ther. 2005 Feb;312(2):742-50. doi: 10.1124/jpet.104.075648. Epub 2004 Oct 14. J Pharmacol Exp Ther. 2005. PMID: 15485895
30 results