[HTML][HTML] CCR5 antagonist TD-0680 uses a novel mechanism for enhanced potency against HIV-1 entry, cell-mediated infection, and a resistant variant
Regardless of the route of transmission, R5-tropic HIV-1 predominates early in infection,
rendering CC chemokine receptor type 5 (CCR5) antagonists as attractive agents not only
for antiretroviral therapy but also for prevention. Here, we report the specificity, potency, and
underlying mechanism of action of a novel small molecule CCR5 antagonist, TD-0680. TD-
0680 displayed the greatest potency against a diverse group of R5-tropic HIV-1 and SIV
strains when compared with its prodrug, TD-0232, the Food and Drug Administration …
rendering CC chemokine receptor type 5 (CCR5) antagonists as attractive agents not only
for antiretroviral therapy but also for prevention. Here, we report the specificity, potency, and
underlying mechanism of action of a novel small molecule CCR5 antagonist, TD-0680. TD-
0680 displayed the greatest potency against a diverse group of R5-tropic HIV-1 and SIV
strains when compared with its prodrug, TD-0232, the Food and Drug Administration …