Format

Send to

Choose Destination
Mol Pharmacol. 2019 Jul 2. pii: mol.119.117168. doi: 10.1124/mol.119.117168. [Epub ahead of print]

Chemokine receptor crystal structures: what can be learnt from them?

Author information

1
Vrije Universiteit Amsterdam; m.arimontsegura@vu.nl r.leus@vu.nl.
2
University Hospital Jena.
3
Sosei Heptares.
4
Vrije Universiteit Amsterdam.

Abstract

Chemokine receptors belong to the class A of G-protein coupled receptors (GPCRs) and are implicated in a wide variety of physiological functions, mostly related to the homeostasis of the immune system. Chemokine receptors are also involved in multiple pathological processes, including immune and autoimmune diseases, as well as cancer. Hence, several members of this GPCR subfamily are considered to be very relevant therapeutic targets. Since drug discovery efforts can be significantly reinforced by the availability of crystal structures, substantial efforts in the area of chemokine receptor structural biology could dramatically increase the outcome of drug discovery campaigns. This short review summarizes the available data on chemokine receptor crystal structures, discusses the numerous applications from chemokine receptor structures that can enhance the daily work of molecular pharmacologists, as well as the challenges and pitfalls to consider when relying on crystal structures for further research applications. SIGNIFICANCE STATEMENT: This short review summarizes the available data on chemokine receptor crystal structures, discusses the numerous applications from chemokine receptor structures that can enhance the daily work of molecular pharmacologists, as well as the challenges and pitfalls to consider when relying on crystal structures for further research applications.

KEYWORDS:

Chemokine receptors; Computational drug design; Drug discovery; G protein-coupled receptors (GPCRs); Receptor structure; X-ray crystallography

PMID:
31266800
DOI:
10.1124/mol.119.117168
Free full text

Supplemental Content

Full text links

Icon for HighWire
Loading ...
Support Center