HIV integrase inhibitor, novel and potent
CAS：1051375-16-6
分子式：C20H19F2N3O5
分子量：419.4
纯度：98%
存储：Store at -20°C

Background:

S/GSK1349572, also known as dolutegravir, is a novel and potent inhibitor of human immunodeficiency virus (HIV) integrase (IN) blocking the strand transfer of integration of the viral genome into the host cell’s DNA. It occupies the physical space in the IN active site of the intasome, contacts with the β4-α2 loop of the catalytic core domain, and enters into the pocket vacated by the displaced viral DNA through its extended linker region connecting the metal chelating core the halobenzyl group.? S/GSK1349572 exhibits potent anti-HIV activity in peripheral blood mononuclear cells (IC50 = 0.51 nM)in vitroand retains activity against raltegravir- and elvitegravir- resistant HIV.

Reference

[1].Sherene Min, Ivy Song, Julie Borland, Shuguang Chen, Yu Lou, Tamio Fujiwara, and Stephen C. Piscitelli. Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY 2010; 54(1): 254-258
[2].Masanori Kobayashi, Tomokazu Yoshinaga, Takahiro Seki, Chiaki Wakasa-Morimoto, Kevin W. Brown, Robert Ferris, Scott A. Foster, Richard J. Hazen, Shigeru Miki, Akemi Suyama-Kagitani, Shinobu Kawauchi-Miki, Teruhiko Taishi, Takashi Kawasuji, Brian A. Johns, Mark R. Underwood, Edward P. Garvey, Akihiko Sato, and Tamio Fujiwara. In vitro antiretroviral prooerties of S/GSK1349572, a next-generation HIV integrase inhibitor. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY 2011; 55(2): 813-821
[3].Stephen Harem Steven J. Smith, Mathieu Metifiot, Albert Jaxa-Chamiec, Yves Pommier, Stephen H. Hughes, and Peter Cherepanov. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol 2011; 80(4): 565-572