title: Direct inactivation of human immunodeficiency virus type 1 by a novel small-molecule entry inhibitor, DCM205.
abstract: With more than 40 million people living with human immunodeficiency virus (HIV), there is an urgent need to develop drugs that can be used in the form of a topical microbicide to prevent infection through sexual transmission. DCM205 is a recently discovered small-molecule inhibitor of HIV type 1 (HIV-1) that is able to directly inactivate HIV-1 in the absence of a cellular target. DCM205 is active against CXCR4-, CCR5-, and dual-tropic laboratory-adapted and primary strains of HIV-1. DCM205 binds to the HIV-1 envelope glycoprotein, and competition studies map the DCM205 binding at or near the V3 loop of gp120. Binding to this site interferes with the soluble CD4 interaction. With its ability to disable the virus particle, DCM205 represents a promising new class of HIV entry inhibitor that can be used as a strategy in the prevention of HIV-1/AIDS.
authors.affiliation: Center for Comparative Medicine, University of California, Davis, Davis, CA 95616, USA.
authors.forename: Yen T
authors.initials: YT
authors.lastname: Duong
authors.forename: D Christopher
authors.initials: DC
authors.lastname: Meadows
authors.forename: Indresh K
authors.initials: IK
authors.lastname: Srivastava
authors.forename: Jacquelyn
authors.initials: J
authors.lastname: Gervay-Hague
authors.forename: Thomas W
authors.initials: TW
authors.lastname: North
mesh_terms: D000163:Acquired Immunodeficiency Syndrome / Q000517:prevention & control / Q000635:transmission; D019380:Anti-HIV Agents / Q000494:pharmacology*; D000891:Anti-Infective Agents, Local / Q000494:pharmacology*; D015704:CD4 Antigens / Q000187:drug effects; D015686:Gene Products, env / Q000378:metabolism; D015699:HIV Envelope Protein gp120 / Q000737:chemistry / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects*; D006367:HeLa Cells; D006801:Humans; D011748:Pyrogallol / Q000031:analogs & derivatives* / Q000494:pharmacology; D013450:Sulfones / Q000494:pharmacology*; D054299:env Gene Products, Human Immunodeficiency Virus
chemical_list: D019380:Anti-HIV Agents; D000891:Anti-Infective Agents, Local; D015704:CD4 Antigens; C520839:DCM 205; D015686:Gene Products, env; D015699:HIV Envelope Protein gp120; D013450:Sulfones; D054299:env Gene Products, Human Immunodeficiency Virus; C097729:gp140 envelope protein, Human immunodeficiency virus 1; D011748:Pyrogallol