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Literature DB >> 24050281

Modeling the allosteric modulation of CCR5 function by Maraviroc.

Bernard Lagane, Javier Garcia-Perez, Esther Kellenberger.

Abstract

Maraviroc is a non-peptidic, low molecular weight CC chemokine receptor 5 (CCR5) ligand that has recently been marketed for the treatment of HIV infected individuals. This review discusses recent molecular modeling studies of CCR5 by homology to CXC chemokine receptor 4, their contribution to the understanding of the allosteric mode of action of the inhibitor and their potential for the development of future drugs with improved efficiency and preservation of CCR5 biological functions.

Entities: Disease Gene

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Year: 2013 PMID： 24050281 DOI： 10.1016/j.ddtec.2012.07.011

Source DB: PubMed Journal: Drug Discov Today Technol ISSN： 1740-6749

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Cited

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4. A single-residue change in the HIV-1 V3 loop associated with maraviroc resistance impairs CCR5 binding affinity while increasing replicative capacity.

Authors: Javier Garcia-Perez; Isabelle Staropoli; Stéphane Azoulay; Jean-Thomas Heinrich; Almudena Cascajero; Philippe Colin; Hugues Lortat-Jacob; Fernando Arenzana-Seisdedos; Jose Alcami; Esther Kellenberger; Bernard Lagane
Journal: Retrovirology Date: 2015-06-18 Impact factor: 4.602

Modeling the allosteric modulation of CCR5 function by Maraviroc.

1. British Pharmacological Society, 5th Focused Meeting on Cell Signalling: Matters arising ….

Review 2. Chemokine and chemokine receptor structure and interactions: implications for therapeutic strategies.

3. Recent Advances on Small-Molecule Survivin Inhibitors

4. A single-residue change in the HIV-1 V3 loop associated with maraviroc resistance impairs CCR5 binding affinity while increasing replicative capacity.

5. Highly specific blockade of CCR5 inhibits leukocyte trafficking and reduces mucosal inflammation in murine colitis.

6. Diazabicyclo analogues of maraviroc: synthesis, modeling, NMR studies and antiviral activity.

7. Chemokine Receptor 5 Antagonism Causes Reduction in Joint Inflammation in a Collagen-Induced Arthritis Mouse Model.