title: Integrase inhibitors for the treatment of HIV infection.
abstract: HIV-1 integrase catalyzes the insertion of HIV-1 DNA into the genome of the host cell and, therefore, represents a rational target for chemotherapeutic intervention in the treatment of HIV-1 infection. Raltegravir, marketed as Isentress, is the first integrase inhibitor to be approved by the FDA for the treatment of HIV AIDS infection. This review briefly describes the successful medicinal chemistry efforts that culminated in the discovery of raltegravir, and highlights more recent progress that has been made in the field of HIV-1 integrase inhibition.
authors.affiliation: IRBM, via Pontina Km 30,600, Pomezia, Rome 00040, Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Pace
authors.forename: Michael
authors.initials: M
authors.lastname: Rowley
mesh_terms: D000818:Animals; D015195:Drug Design; D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D019428:HIV Integrase Inhibitors / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D006801:Humans; D015394:Molecular Structure; D011760:Pyrrolidinones / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D000068898:Raltegravir Potassium; D016896:Treatment Outcome
chemical_list: D019428:HIV Integrase Inhibitors; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium