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Page 1
Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.
Wu YJ, Davis CD, Dworetzky S, Fitzpatrick WC, Harden D, He H, Knox RJ, Newton AE, Philip T, Polson C, Sivarao DV, Sun LQ, Tertyshnikova S, Weaver D, Yeola S, Zoeckler M, Sinz MW. Wu YJ, et al. Among authors: tertyshnikova s. J Med Chem. 2003 Aug 28;46(18):3778-81. doi: 10.1021/jm034111v. J Med Chem. 2003. PMID: 12930139
(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.
Wu YJ, Boissard CG, Greco C, Gribkoff VK, Harden DG, He H, L'Heureux A, Kang SH, Kinney GG, Knox RJ, Natale J, Newton AE, Lehtinen-Oboma S, Sinz MW, Sivarao DV, Starrett JE Jr, Sun LQ, Tertyshnikova S, Thompson MW, Weaver D, Wong HS, Zhang L, Dworetzky SI. Wu YJ, et al. Among authors: tertyshnikova s. J Med Chem. 2003 Jul 17;46(15):3197-200. doi: 10.1021/jm034073f. J Med Chem. 2003. PMID: 12852750
Chemical genetics reveals an RGS/G-protein role in the action of a compound.
Fitzgerald K, Tertyshnikova S, Moore L, Bjerke L, Burley B, Cao J, Carroll P, Choy R, Doberstein S, Dubaquie Y, Franke Y, Kopczynski J, Korswagen H, Krystek SR, Lodge NJ, Plasterk R, Starrett J, Stouch T, Thalody G, Wayne H, van der Linden A, Zhang Y, Walker SG, Cockett M, Wardwell-Swanson J, Ross-Macdonald P, Kindt RM. Fitzgerald K, et al. Among authors: tertyshnikova s. PLoS Genet. 2006 Apr;2(4):e57. doi: 10.1371/journal.pgen.0020057. Epub 2006 Apr 21. PLoS Genet. 2006. PMID: 16683034 Free PMC article.
Evaluation and optimization of compound solubilization and delivery methods in a two-tiered ion channel lead optimization triage.
Hendricson AW, Gallagher L, Matchett M, Ferrante M, Spence S, Paiva T, Shou W, Tertyshnikova S, Krambis M, Post-Munson D, Zhang L, Knox R. Hendricson AW, et al. Among authors: tertyshnikova s. Assay Drug Dev Technol. 2012 Apr;10(2):202-11. doi: 10.1089/adt.2011.0385. Epub 2011 Nov 15. Assay Drug Dev Technol. 2012. PMID: 22085018
14 results