Proc. Natl. Acad. Sci. USA
A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding.
Lin, P.F., Blair, W., Wang, T., Spicer, T., Guo, Q., Zhou, N., Gong, Y.F., Wang, H.G., Rose, R., Yamanaka, G., Robinson, B., Li, C.B., Fridell, R., Deminie, C., Demers, G., Yang, Z., Zadjura, L., Meanwell, N. and Colonno, R.
Notes: To test the effect of BMS-378806, a new small molecule inhibitor of HIV-1, a cell fusion assay was developed. Target cells that stably expressed CD4, CXCR4 or CCR5 receptors and carry a responsive luciferase plasmid were prepared. Effector cells were transiently transfected with HIV coat protein gp160 from various strains of virus, and a plasmid to activate the responsive element promoting luciferase. Therefore, if the cells fuse, luciferase is activated. To measure this activation, effector cells were plated with target cells in a 1:2 ratio and seeded into 96-well plates at 1.5 x 104 cells/well and incubated with various concentrations of BMS-378806 for 12-24 hours. Luciferase activity was determined with the Steady-Glo® Reagent. (2737)
Expand Full Notes »