Description
BMS 626529 is an inhibitor of HIV-1 attachment.
1,2 It binds to non-ligand bound HIV-1 gp120 to inhibit HIV-1 interaction with host CD4
+ T cells and subsequent HIV-1 binding and cell entry.
1 BMS 626529 reduces infectivity of laboratory strains and clinical isolates of HIV-1 (EC
50s = 0.4-2,000 and 25-2,000 nM, respectively) with cytotoxic concentration (CC
50) values greater than 100 μM in a panel of mammalian cell lines.
2
in vitro
the activity of bms-626529 is virus dependent, due to heterogeneity within gp120. bms-626529 had half-maximal effective concentration values of6 log10, with half-maximal effective concentration values in the low pm range against the most susceptible viruses. measurement of the binding affinity of bms-626529 for purified gp120 suggests that a contributory factor to its inhibitory potency may be a relatively long dissociative half-life [1].
References
[1] nowicka-sans b, gong yf, mcauliffe b, dicker i, ho ht, zhou n, eggers b, lin pf, ray n, wind-rotolo m, zhu l, majumdar a, stock d, lataillade m, hanna gj, matiskella jd, ueda y, wang t, kadow jf, meanwell na, krystal m. in vitro antiviral characteristics of hiv-1 attachment inhibitor bms-626529, the active component of the prodrug bms-663068. antimicrob agents chemother. 2012;56(7):3498-507.
[2] nettles re, schürmann d, zhu l, stonier m, huang sp, chang i, chien c, krystal m, wind-rotolo m, ray n, hanna gj, bertz r, grasela d. pharmacodynamics, safety, and pharmacokinetics of bms-663068, an oral hiv-1 attachment inhibitor in hiv-1-infected subjects. j infect dis. 2012;206(7):1002-11.
