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.