Article
The naphthyridinone GSK364735 is a novel, potent human immunodeficiency virus type 1 integrase inhibitor and antiretroviral.
Antimicrobial agents and chemotherapy - 1 Mar 2008
Garvey Edward P, Johns Brian A, Gartland Margaret J, Foster Scott A, Miller Wayne H, Ferris Robert G, Hazen Richard J, Underwood Mark R, Boros Eric E, Thompson James B, Weatherhead Jason G, Koble Cecilia S, Allen Scott H, Schaller Lee T, Sherrill Ronald G, Yoshinaga Tomokazu, Kobayashi Masanori, Wakasa-Morimoto Chiaki, Miki Shigeru, Nakahara Koichiro, Noshi Takeshi, Sato Akihiko, Fujiwara Tamio
Abstract excerpt
The naphthyridinone GSK364735 potently inhibited recombinant human immunodeficiency virus type 1 (HIV-1) integrase in a strand transfer assay (mean 50% inhibitory concentration +/- standard deviation, 8 +/- 2 nM). As expected based on the structure of the drug, it bound competitively with another two-metal binding inhibitor (Kd [binding constant], 6 +/- 4 nM). In a number of different cellular assays, GSK364735...
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