Chemokine receptors in GtoPdb v.2025.1

Chemokine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Chemokine Receptors [459, 458, 32]) comprise a large subfamily of 7TM proteins that bind one or more chemokines, a large family of small cytokines typically possessing chemotactic activity for leukocytes. Additional hematopoietic and non-hematopoietic roles have been identified for many chemokines in the areas of embryonic development, immune cell proliferation, activation and death, viral infection, and as antibacterials, among others. Chemokine receptors can be divided by function into two main groups: G protein-coupled chemokine receptors, which mediate leukocyte trafficking, and "Atypical chemokine receptors", which may signal through non-G protein-coupled mechanisms and act as chemokine scavengers to downregulate inflammation or shape chemokine gradients [32].Chemokines in turn can be divided by structure into four subclasses by the number and arrangement of conserved cysteines. CC (also known as β-chemokines; n= 28), CXC (also known as α-chemokines; n= 17) and CX3C (n= 1) chemokines all have four conserved cysteines, with zero, one and three amino acids separating the first two cysteines respectively. C chemokines (n= 2) have only the second and fourth cysteines found in other chemokines. Chemokines can also be classified by function into homeostatic and inflammatory subgroups. Most chemokine receptors are able to bind multiple high-affinity chemokine ligands, but the ligands for a given receptor are almost always restricted to the same structural subclass. Most chemokines bind to more than one receptor subtype. Receptors for inflammatory chemokines are typically highly promiscuous with regard to ligand specificity, and may lack a selective endogenous ligand. G protein-coupled chemokine receptors are named acccording to the class of chemokines bound, whereas ACKR is the root acronym for atypical chemokine receptors [33]. There can be substantial cross-species differences in the sequences of both chemokines and chemokine receptors, and in the pharmacology and biology of chemokine receptors. Endogenous and microbial non-chemokine ligands have also been identified for chemokine receptors. Many chemokine receptors function as HIV co-receptors, but CCR5 is the only one demonstrated to play an essential role in HIV/AIDS pathogenesis. The tables include both standard chemokine receptor names [717] and aliases.

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IUPHAR/BPS Guide to Pharmacology CITE
Published
2025-04-01
DOI
https://doi.org/10.2218/gtopdb/f14/2025.1
Primary Topic
Chemokine receptors and signaling
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article
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article

Chemokine receptors in GtoPdb v.2025.1

Rebecca Hills, Kouji Matsushima, Massimo Locati, Antal Rot et al.
IUPHAR/BPS Guide to Pharmacology CITE
Chemokine receptors and signaling
article

Chemokine receptors in GtoPdb v.2025.1

Rebecca Hills, Kouji Matsushima, Massimo Locati, Antal Rot, Marcus Thelen, Hisayuki Nomiyama, Gerard J. Graham, Adit Ben‐Baruch, Amanda M. Burkhardt, METTE MARIE ROSENKILDE, Reinhold Förster, Joost J. Oppenheim, Amy E. Monaghan, Osamu Yoshie, Alberto Mantovani, Silvano Sozzani, Andrew D. Luster, Joshua Μ. Farber, Alexander H. Sparre‐Ulrich, Richard Horuk, Françoise Bachelerie, Philip M. Murphy, Mohib Uddin, Christophe Combadière, Robert J. B. Nibbs, Albert Zlotnik, Christine A. Power, Georgios L. Moschovakis, Amanda E. I. Proudfoot, Israel Charo
article en

Abstract

Chemokine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Chemokine Receptors [459, 458, 32]) comprise a large subfamily of 7TM proteins that bind one or more chemokines, a large family of small cytokines typically possessing chemotactic activity for leukocytes. Additional hematopoietic and non-hematopoietic roles have been identified for many chemokines in the areas of embryonic development, immune cell proliferation, activation and death, viral infection, and as antibacterials, among others. Chemokine receptors can be divided by function into two main groups: G protein-coupled chemokine receptors, which mediate leukocyte trafficking, and "Atypical chemokine receptors", which may signal through non-G protein-coupled mechanisms and act as chemokine scavengers to downregulate inflammation or shape chemokine gradients [32].Chemokines in turn can be divided by structure into four subclasses by the number and arrangement of conserved cysteines. CC (also known as β-chemokines; n= 28), CXC (also known as α-chemokines; n= 17) and CX3C (n= 1) chemokines all have four conserved cysteines, with zero, one and three amino acids separating the first two cysteines respectively. C chemokines (n= 2) have only the second and fourth cysteines found in other chemokines. Chemokines can also be classified by function into homeostatic and inflammatory subgroups. Most chemokine receptors are able to bind multiple high-affinity chemokine ligands, but the ligands for a given receptor are almost always restricted to the same structural subclass. Most chemokines bind to more than one receptor subtype. Receptors for inflammatory chemokines are typically highly promiscuous with regard to ligand specificity, and may lack a selective endogenous ligand. G protein-coupled chemokine receptors are named acccording to the class of chemokines bound, whereas ACKR is the root acronym for atypical chemokine receptors [33]. There can be substantial cross-species differences in the sequences of both chemokines and chemokine receptors, and in the pharmacology and biology of chemokine receptors. Endogenous and microbial non-chemokine ligands have also been identified for chemokine receptors. Many chemokine receptors function as HIV co-receptors, but CCR5 is the only one demonstrated to play an essential role in HIV/AIDS pathogenesis. The tables include both standard chemokine receptor names [717] and aliases.

IUPHAR/BPS Guide to Pharmacology CITEVol. 2025(1)
University of Copenhagen (DK), National Institutes of Health (US), Gladstone Institutes (US), Inserm (FR), Institut Pasteur (FR), Tel Aviv University (IL), University of Milan (IT), University of California, Irvine (US), Brescia University (US), Medizinische Hochschule Hannover (DE), Massachusetts General Hospital (US), Merck Serono S.A. (Switzerland) (CH), AstraZeneca (Brazil) (BR), Frederick National Laboratory for Cancer Research (US), National Institute of Allergy and Infectious Diseases (US), The University of Tokyo (JP), University of Glasgow (GB), University of Birmingham (GB), University of Brescia (IT), Kindai University (JP), Kumamoto University (JP), University of Edinburgh (GB)
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Chemokine receptors and signaling
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