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 12月 2021
Accepted
04 3月 2022
First published
07 3月 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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements