Abstract

BMS-378806 is a newly described small-molecule inhibitor of human immunodeficiency virus type 1 (HIV-1) replication. It acts by binding to the gp120 surface glycoprotein of the virus within, or very close to, the pocket normally occupied by the CD4 antigen, the primary cell-surface receptor protein of HIV-1. Consequently, BMS-378806 inhibits gp120–CD4 binding and the subsequent events of virus–cell attachment and fusion. Thus, BMS-378806 or a derivative could be highly suitable to treat HIV-1 infection, and perhaps also to prevent infection when used in combination with other inhibitors of HIV-1 entry.

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