Issue 26, 2022

Targeting chemokine receptors from the inside-out: discovery and development of small-molecule intracellular antagonists

Abstract

Ever since the first biologically active chemokines were discovered in the late 1980s, these messenger proteins and their receptors have been the target for a plethora of drug discovery efforts in the pharmaceutical industry, as well as in academia. Owing to the publication of several chemokine receptor X-ray crystal structures, a highly druggable, intracellular, allosteric binding site which partially overlaps with the G protein binding site was discovered. This intriguing, new approach for chemokine receptor antagonism has captured researchers around the world, pushing the exploration of this intracellular binding site and new antagonists thereof. In this review, we have highlighted the past two decades of research on small-molecule chemokine receptor antagonists that modulate receptor function at the intracellular binding site.

Graphical abstract: Targeting chemokine receptors from the inside-out: discovery and development of small-molecule intracellular antagonists

Article information

Article type
Highlight
Submitted
16 Dec. 2021
Accepted
04 Marts 2022
First published
07 Marts 2022

Chem. Commun., 2022,58, 4132-4148

Targeting chemokine receptors from the inside-out: discovery and development of small-molecule intracellular antagonists

M. Billen, D. Schols and P. Verwilst, Chem. Commun., 2022, 58, 4132 DOI: 10.1039/D1CC07080K

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