BMS-806 is a small molecule that inhibits the first step of HIV-1 infection by blocking the binding of host cell CD4 with viral gp120 protein. It binds the exterior envelope glycoprotein gp120 (Kd= 21.1 nM; Ki = 24.9 nM), blocking the conformational change that occurs with CD4 binding and preventing fusion of the viral and target cell membranes. BMS-806 is specific to HIV-1 irrespective of chemokine receptor preference, with no activity against HIV-2, SIV, or a panel of additional viruses.
[1] wang t1, zhang z, wallace ob, deshpande m, fang h, yang z, zadjura lm, tweedie dl, huang s, zhao f, ranadive s, robinson bs, gong yf, ricarrdi k, spicer tp, deminie c, rose r, wang hg, blair ws, shi py, lin pf, colonno rj, meanwell na. discovery of 4-benzoyl-1-[(4-methoxy-1h- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (r)-methylpiperazine (bms-378806): a novel hiv-1 attachment inhibitor that interferes with cd4-gp120 interactions. j med chem. 2003 sep 25;46(20):4236-9.
