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Discovery of Potent HIV-1 Capsid Assembly Inhibitors
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Reported by Jules Levin
17th CROI, Feb 16-19 2010 SF
Steve Titolo1, Jean-François Mercier1, Elizabeth Wardrop1, Utavon Schwedler3, Nathalie Goudreau2, Chris Lemke2, Anne-Marie Faucher2, ChristianeYoakim2, Bruno Simoneau2, Wesley I. Sundquist3, Stephen Mason1
Boehringer Ingelheim (Canada) Ltd. Research & Development, Laval, Québec, Canada: 1Departments of Biological Sciences and 2Chemistry; 3Biochemistry Department, University of Utah, Salt Lake City, Utah, U.S.A.
from Jules: there was very little in the way of new drug discovery presented at CROI regarding new targets. The GSK integrase & the Gilead integrase programs are moving ahead, Tobira updated on their CCR5. Tibotec has TMC278 development ongoing.
Mason said "Assembly & stability of the capsid core is absolutely essential for HIV infectivity....in the presence of inhibitors the formation of the complexes is prevented....several hits were obtained....two chemotypes of advanced leads were identified that potently inhibit capsid assembly, with 2 different modes of action....mode of action is consistent with inhibition of capsid assembly....inhibitors are active in very late phase of viral replication which is also consistent with an effect on capsid assembly and viral replication....resistance mutations may indicate high genetic barrier to resistance....lead optimization was terminated, inihibition of capsid assembly is a potential viable approach for antiretroviral intervention"
http://app2.capitalreach.com/esp1204/servlet/tc?c=10164&cn=retro&e=12343&m=1&s=20431&&espmt=2&mp3file=12343&m4bfile=12343
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