A novel small-molecular CCR5 antagonist promotes neural repair after stroke.

ABSTRACT: Chemokine receptor 5 (CCR5) is one of the main co-receptors of HIV-1, and has been found to be a potential therapeutic target for stroke. Maraviroc is a classic CCR5 antagonist, which is undergoing clinical trials against stroke. As maraviroc shows poor blood-brain barrier (BBB) permeability, it is of interest to find novel CCR5 antagonists suitable for neurological medication. In this study we characterized the therapeutic potential of a novel CCR5 antagonist A14 in treating ischemic stroke mice. A14 was discovered in screening millions compounds in the Chemdiv library based on the molecular docking diagram of CCR5 and maraviroc. We found that A14 dose-dependently inhibited the CCR5 activity with an IC₅₀ value of 4.29 μM. Pharmacodynamic studies showed that A14 treatment exerte

SUBMITTER: Wu QL 

PROVIDER: S-EPMC10545720 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature