CCR5/CXCR4 Dual Antagonism for the Improvement of HIV Infection Therapy.

Fedora Grande, Maria Antonietta Occhiuzzi, Bruno Rizzuti, Giuseppina Ioele, Michele De Luca, Paola Tucci, Valentina Svicher, Stefano Aquaro, Antonio Garofalo

Journal: Molecules (Basel, Switzerland) 2019;24(3):550

PMID: 30717348

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Abstract

HIV entry in the host cell requires the interaction with the CD4 membrane receptor, and depends on the activation of one or both co-receptors CCR5 and CXCR4. Former selective co-receptor antagonists, acting at early stages of infection, are able to impair the receptor functions, preventing the viral spread toward AIDS. Due to the capability of HIV to develop resistance by switching from CCR5 to CXCR4, dual co-receptor antagonists could represent the next generation of AIDS prophylaxis drugs. We herein present a survey on relevant results published in the last few years on compounds acting simultaneously on both co-receptors, potentially useful as preventing agents or in combination with classical anti-retroviral drugs based therapy.

Address: Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampliamento Polifunzionale, Via P. Bucci, 87036 Rende (CS), Italy. [email protected].; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampliamento Polifunzionale, Via P. Bucci, 87036 Rende (CS), Italy. [email protected].; CNR-NANOTEC, Licryl-UOS Cosenza and CEMIF.Cal, Department of Physics, University of Calabria, Via P. Bucci, 87036 Rende (CS), Italy. [email protected].; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampliamento Polifunzionale, Via P. Bucci, 87036 Rende (CS), Italy. [email protected].; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampliamento Polifunzionale, Via P. Bucci, 87036 Rende (CS), Italy. [email protected].; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampliamento Polifunzionale, Via P. Bucci, 87036 Rende (CS), Italy. [email protected].; Department of Experimental Medicine, University of Rome "Tor Vergata", 00133 Rome, Italy. [email protected].; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampliamento Polifunzionale, Via P. Bucci, 87036 Rende (CS), Italy. [email protected].; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ampliamento Polifunzionale, Via P. Bucci, 87036 Rende (CS), Italy. [email protected].

DOI: 10.3390/molecules24030550

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Medical:

https://medlineplus.gov/hivmedicines.html

Research Materials:

https://antibodies.cancer.gov/detail/CPTC-CD4-1

MeSH Terms: Anti-HIV Agents, Benzylamines, CCR5 Receptor Antagonists, Cyclams, HIV Infections, HIV-1, Heterocyclic Compounds, Humans, Maraviroc, Pyridines, Receptors, CCR5, Receptors, CXCR4