title: Dimerization inhibitors of HIV-1 reverse transcriptase, protease and integrase: a single mode of inhibition for the three HIV enzymes?
abstract: The genome of human immunodeficiency virus type 1 (HIV-1) encodes 15 distinct proteins, three of which provide essential enzymatic functions: a reverse transcriptase (RT), an integrase (IN), and a protease (PR). Since these enzymes are all homodimers, pseudohomodimers or multimers, disruption of protein-protein interactions in these retroviral enzymes may constitute an alternative way to achieve HIV-1 inhibition. A growing number of dimerization inhibitors for these enzymes is being reported. This mini review summarizes some approaches that have been followed for the development of compounds that inhibit those three enzymes by interfering with the dimerization interfaces between the enzyme subunits.
authors.affiliation: Instituto de Química Médica (C.S.I.C.), Juan de la Cierva 3, 28006 Madrid, Spain. mj.camarasa@iqm.csic.es
authors.forename: María-José
authors.initials: MJ
authors.lastname: Camarasa
authors.forename: Sonsoles
authors.initials: S
authors.lastname: Velázquez
authors.forename: Ana
authors.initials: A
authors.lastname: San-Félix
authors.forename: María-Jesús
authors.initials: MJ
authors.lastname: Pérez-Pérez
authors.forename: Federico
authors.initials: F
authors.lastname: Gago
mesh_terms: D019380:Anti-HIV Agents / Q000494:pharmacology*; D019281:Dimerization; D015195:Drug Design; D019427:HIV Integrase / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D016333:HIV Protease / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D006801:Humans; D008958:Models, Molecular; D018894:Reverse Transcriptase Inhibitors / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D018894:Reverse Transcriptase Inhibitors; D019427:HIV Integrase; D054303:HIV Reverse Transcriptase; D016333:HIV Protease