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Research ArticleMinireview

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

Marta Arimont, Carsten Hoffmann, Chris de Graaf and Rob Leurs
Molecular Pharmacology July 2, 2019, mol.119.117168; DOI: https://doi.org/10.1124/mol.119.117168
Marta Arimont
1 Vrije Universiteit Amsterdam;
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Carsten Hoffmann
2 University Hospital Jena;
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Chris de Graaf
3 Sosei Heptares
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Rob Leurs
1 Vrije Universiteit Amsterdam;
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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.

  • Chemokine receptors
  • Computational drug design
  • Drug discovery
  • G protein-coupled receptors (GPCRs)
  • Receptor structure
  • X-ray crystallography
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 102 (2)
Molecular Pharmacology
Vol. 102, Issue 2
1 Aug 2022
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Research ArticleMinireview

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

Marta Arimont, Carsten Hoffmann, Chris de Graaf and Rob Leurs
Molecular Pharmacology July 2, 2019, mol.119.117168; DOI: https://doi.org/10.1124/mol.119.117168

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Research ArticleMinireview

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

Marta Arimont, Carsten Hoffmann, Chris de Graaf and Rob Leurs
Molecular Pharmacology July 2, 2019, mol.119.117168; DOI: https://doi.org/10.1124/mol.119.117168
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