title: Inhibition of the interaction between HIV-1 integrase and its cofactor LEDGF/p75: a promising approach in anti-retroviral therapy.
abstract: Although 25 compounds are currently licensed as anti-HIV drugs, the development of multidrug-resistant viruses, as well as their severe side effects, compromise their efficacy and limit treatment options. The search for new targets in order to cure AIDS has revealed that the inhibition of some protein-protein interactions in the HIV life cycle may provide an important new approach to fight this disease. The interaction between HIV-1 integrase (IN) and Lens Epithelium-Derived Growth Factor (LEDGF/p75) has increasingly gained attention as a valuable target for a novel anti-retroviral strategy. This article reviews the discovery and development of molecules capable of interrupting the LEDGF/p75-IN interaction reported to date.
authors.affiliation: Dipartimento Farmaco-Chimico, Università degli Studi di Messina, Italy. ldeluca@unime.it
authors.forename: L
authors.initials: L
authors.lastname: De Luca
authors.forename: S
authors.initials: S
authors.lastname: Ferro
authors.forename: F
authors.initials: F
authors.lastname: Morreale
authors.forename: A
authors.initials: A
authors.lastname: Chimirri
mesh_terms: D001565:Benzoates / Q000737:chemistry / Q000494:pharmacology; D003374:Coumarins / Q000737:chemistry / Q000494:pharmacology; D019427:HIV Integrase / Q000737:chemistry* / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000494:pharmacology; D036341:Intercellular Signaling Peptides and Proteins / Q000737:chemistry* / Q000378:metabolism; D010456:Peptides, Cyclic / Q000737:chemistry / Q000494:pharmacology; D017434:Protein Structure, Tertiary; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology
chemical_list: D001565:Benzoates; D003374:Coumarins; D019428:HIV Integrase Inhibitors; D007211:Indoles; D036341:Intercellular Signaling Peptides and Proteins; D010456:Peptides, Cyclic; D011804:Quinolines; C119380:lens epithelium-derived growth factor; C037219:quinoline; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1