Article
Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572).
Molecular pharmacology - 1 Oct 2011
Hare Stephen, Smith Steven J, Métifiot Mathieu, Jaxa-Chamiec Albert, Pommier Yves, Hughes Stephen H, Cherepanov Peter
Abstract excerpt
Raltegravir (RAL) and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs) efficiently block viral replication in vitro and suppress viremia in patients. These small molecules bind to the IN active site, causing it to disengage from the deoxyadenosine at the 3' end of viral DNA. The emergence of viral strains that are highly resistant to RAL underscores the pressing need to develop INSTIs with...
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