Filling the Gaps in Antagonist CCR5 Binding, a Retrospective and Perspective Analysis.

ABSTRACT: The large number of pathologies that position CCR5 as a central molecular determinant substantiates the studies aimed at understanding receptor-ligand interactions, as well as the development of compounds that efficiently block this receptor. This perspective focuses on CCR5 antagonism as the preferred landscape for therapeutic intervention, thus the receptor active site occupancy by known antagonists of different origins is overviewed. CCL5 is a natural agonist ligand for CCR5 and an extensively studied scaffold for CCR5 antagonists production through chemokine N-terminus modification. A retrospective 3D modeling analysis on recently developed CCL5 mutants and their contribution to enhanced anti-HIV-1 activity is reported here. These results allow us to prospect the development of concept

SUBMITTER: Amerzhanova Y 

PROVIDER: S-EPMC8807524 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature