title: HIV-1 IN inhibitors: 2010 update and perspectives.
abstract: Integrase (IN) is the newest validated target against AIDS and retroviral infections. The remarkable activity of raltegravir (Isentress((R))) led to its rapid approval by the FDA in 2007 as the first IN inhibitor. Several other IN strand transfer inhibitors (STIs) are in development with the primary goal to overcome resistance due to the rapid occurrence of IN mutations in raltegravir-treated patients. Thus, many scientists and drug companies are actively pursuing clinically useful IN inhibitors. The objective of this review is to provide an update on the IN inhibitors reported in the last two years, including second generation STI, recently developed hydroxylated aromatics, natural products, peptide, antibody and oligonucleotide inhibitors. Additionally, the targeting of IN cofactors such as LEDGF and Vpr will be discussed as novel strategies for the treatment of AIDS.
authors.affiliation: Laboratory of Molecular Pharmacology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA.
authors.forename: Christophe
authors.initials: C
authors.lastname: Marchand
authors.forename: Kasthuraiah
authors.initials: K
authors.lastname: Maddali
authors.forename: Mathieu
authors.initials: M
authors.lastname: Métifiot
authors.forename: Yves
authors.initials: Y
authors.lastname: Pommier
mesh_terms: D024882:Drug Resistance, Viral; D019428:HIV Integrase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000201:enzymology*; D008958:Models, Molecular
chemical_list: D019428:HIV Integrase Inhibitors