Article
Dolutegravir (S/GSK1349572) exhibits significantly slower dissociation than raltegravir and elvitegravir from wild-type and integrase inhibitor-resistant HIV-1 integrase-DNA complexes.
Antimicrobial agents and chemotherapy - 1 Oct 2011
Hightower Kendra E, Wang Ruolan, Deanda Felix, Johns Brian A, Weaver Kurt, Shen Yingnian, Tomberlin Ginger H, Carter H Luke, Broderick Timothy, Sigethy Scott, Seki Takahiro, Kobayashi Masanori, Underwood Mark R
Abstract excerpt
The integrase inhibitor (INI) dolutegravir (DTG; S/GSK1349572) has significant activity against HIV-1 isolates with raltegravir (RAL)- and elvitegravir (ELV)-associated resistance mutations. As an initial step in characterizing the different resistance profiles of DTG, RAL, and ELV, we determined the dissociation rates of these INIs with integrase (IN)-DNA complexes containing a broad panel of IN proteins,...
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