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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. 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
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. 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. 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.
Intratumoral IL12 mRNA Therapy Promotes TH1 Transformation of the Tumor Microenvironment.
Hewitt SL, Bailey D, Zielinski J, Apte A, Musenge F, Karp R, Burke S, Garcon F, Mishra A, Gurumurthy S, Watkins A, Arnold K, Moynihan J, Clancy-Thompson E, Mulgrew K, Adjei G, Deschler K, Potz D, Moody G, Leinster DA, Novick S, Sulikowski M, Bagnall C, Martin P, Lapointe JM, Si H, Morehouse C, Sedic M, Wilkinson RW, Herbst R, Frederick JP, Luheshi N. Hewitt SL, et al. Clin Cancer Res. 2020 Dec 1;26(23):6284-6298. doi: 10.1158/1078-0432.CCR-20-0472. Epub 2020 Aug 17. Clin Cancer Res. 2020. PMID: 32817076
49 results