Integrase inhibitors to treat HIV/AIDS.
HIV integrase is a rational target for treating HIV infection and preventing AIDS. It took approximately 12 years to develop clinically usable inhibitors of integrase, and Phase I clinical trials of integrase inhibitors have just begun. This review focuses on the molecular basis and rationale for developing integrase inhibitors. The main classes of lead compounds are also described, as well as the concept of interfacial inhibitors of protein-nucleic-acid interactions that might apply to the clinically used strand-transfer inhibitors.
Pommier
Yves
Y
Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA.
Johnson
Allison A
AA
Marchand
Christophe
C
D017954:Africa South of the Sahara / Q000453:epidemiology; D023241:Antiretroviral Therapy, Highly Active / Q000009:adverse effects; D017277:Drug Approval; D006678:HIV / Q000502:physiology*; D015658:HIV Infections / Q000188:drug therapy* / Q000453:epidemiology / Q000401:mortality; D019428:HIV Integrase Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D006801:Humans; D009154:Mutation; D013329:Structure-Activity Relationship; D014481:United States; D014486:United States Food and Drug Administration; D014779:Virus Replication / Q000187:drug effects / Q000502:physiology
D019428:HIV Integrase Inhibitors