Integrase inhibitors for the treatment of HIV infection.
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.
Pace
Paola
P
IRBM, via Pontina Km 30,600, Pomezia, Rome 00040, Italy.
Rowley
Michael
M
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
D019428:HIV Integrase Inhibitors; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium