The chemokine receptor CCR5 plays a crucial role in transmission of HIV isolates, which predominate in the early and middle stages of infection. DAPTA is a non-toxic experimental antiviral entry inhibitor by selectively targeting CCR5 with potent anti-HIV activities. DAPTA potently inhibited specific CD4-dependent binding of gp120 Bal and CM235 to CCR5 with IC50s of 0.06 nM and 0.32 nM, respectively. DAPTA inhibited the binding of gp120BaL/sCD4 to CCR5 in Cf2Th/synR5 cells with an IC50 of 55 pM. In immunoprecipitation assay, DAPTA (1 nM) blocked the formation of gp120/sCD4 complex with CCR5[1]. DAPTA increased the Th2 cytokines IL-4, IL-10, and IL-13 and induced a potent virostatic state in infected macrophages in vitro, as well as inhibited production of the proinflammatory cytokines IL-1 and TNFα, which upregulate virus expression[2].
United States, District of Col... 展开 >>umbia
Whitman Walker Clinic
Recruiting
Washington, District of Columbia, United States, 20009
Principal Investigator: Richard Elion, MD 收起 <<
United States, District of Col... 展开 >>umbia
Whitman Walker Clinic
Recruiting
Washington, District of Columbia, United States, 20009
Principal Investigator: Richard Elion, MD 收起 <<
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