Mini Rev Med Chem. 2011 Jul;11(8):714-27.

Inhibition of the interaction between HIV-1 integrase and its cofactor LEDGF/p75: a promising approach in anti-retroviral therapy.

De Luca L, Ferro S, Morreale F, Chimirri A.

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Dipartimento Farmaco-Chimico, Università degli Studi di Messina, Italy. ldeluca@unime.it

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.

PMID:: 21651465; [PubMed - indexed for MEDLINE]

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Review Inhibitors of the interactions between HIV-1 IN and the cofactor LEDGF/p75. [ChemMedChem. 2011]
Review Inhibitors of the interactions between HIV-1 IN and the cofactor LEDGF/p75.
De Luca L, Ferro S, Morreale F, De Grazia S, Chimirri A. ChemMedChem. 2011 Jul 4; 6(7):1184-91. Epub 2011 Apr 19.
Pharmacophore-based discovery of small-molecule inhibitors of protein-protein interactions between HIV-1 integrase and cellular cofactor LEDGF/p75. [ChemMedChem. 2009]
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De Luca L, Barreca ML, Ferro S, Christ F, Iraci N, Gitto R, Monforte AM, Debyser Z, Chimirri A. ChemMedChem. 2009 Aug; 4(8):1311-6.
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De Luca L, Ferro S, Gitto R, Barreca ML, Agnello S, Christ F, Debyser Z, Chimirri A. Bioorg Med Chem. 2010 Nov 1; 18(21):7515-21. Epub 2010 Sep 17.
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Cited by 1 PubMed Central article

Novel therapeutic strategies targeting HIV integrase. [BMC Med. 2012]
Novel therapeutic strategies targeting HIV integrase.
Quashie PK, Sloan RD, Wainberg MA. BMC Med. 2012 Apr 12; 10:34. Epub 2012 Apr 12.

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Inhibition of the interaction between HIV-1 integrase and its cofactor LEDGF/p75: a promising approach in anti-retroviral therapy.

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