Chemokine receptors

Overview

Chemokine receptors 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 antibiotics, 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 [1].

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 [2]. 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 [3] and aliases.

References

  1. Bachelerie F, Ben-Baruch A, Burkhardt AM, et al. International Union of Pharmacology. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors. Pharmacol Rev 2014;66:1-79.
  2. Bachelerie F, Graham GJ, Locati M, et al. An atypical addition to the chemokine receptor nomenclature: IUPHAR Review 15. Br J Pharmacol 2015;172:3945-9.
  3. Zlotnik A, Yoshie O. Chemokines: a new classification system and their role in immunity. Immunity 2000;12:121-7.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Human
Available
Assay modes:
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250 pM
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Reference agonist:
CCL2
EC50:
1.3 nM
Human
Available
Assay modes:
Agonist
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Human non-orphan GPCRs
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Reference agonist:
CCL22
EC50:
20 nM
Human
Available
Assay modes:
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Antagonist
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Human non-orphan GPCRs
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Reference agonist:
CCL4
EC50:
7.1 nM
Human
Available
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Human non-orphan GPCRs
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Reference agonist:
CCL20
EC50:
3.8 nM
Human
Available
Assay modes:
Agonist
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Antagonist
PAM
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Human non-orphan GPCRs
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Reference agonist:
CCL21
EC50:
15 nM
Human
Available
Assay modes:
Agonist
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Antagonist
PAM
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Human non-orphan GPCRs
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Reference agonist:
CCL1
EC50:
6.8 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
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Panels:
Human non-orphan GPCRs
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Reference agonist:
CCL25
EC50:
15 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Hematology
à la carte
Reference agonist:
CCL27
EC50:
27 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Gastrointestinal
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Reference agonist:
CXCL6
EC50:
20 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
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Hematology
Neurology
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Reference agonist:
CXCL6
EC50:
27 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
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Reference agonist:
CXCL11
EC50:
29 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Oncology
Hematology
Endocrinology/Metabolism
Neurology
Ophthalmology
Cardiology
Respiratory
Gastrointestinal
Dermatology
Musculoskeletal
Urology/Reproduction
à la carte
Reference agonist:
cXCL12a
EC50:
5.4 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Hematology
Ophthalmology
Gastrointestinal
Dermatology
Musculoskeletal
à la carte
Reference agonist:
CXCL13
EC50:
36 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Oncology
Hematology
Ophthalmology
Cardiology
Respiratory
Gastrointestinal
Dermatology
Musculoskeletal
Urology/Reproduction
à la carte
Reference agonist:
CXCL16
EC50:
3.9 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
-
Reference agonist:
XCL1
EC50:
43 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Hematology
Neurology
Ophthalmology
Cardiology
Respiratory
Gastrointestinal
Dermatology
Musculoskeletal
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à la carte
Reference agonist:
CX3CL1
EC50:
1.8 nM
Human
Assay modes:
-
Panels:
-
Reference agonist:
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CCL3
EC50:
550 pM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CCL22
EC50:
7.9 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CCL4
EC50:
3.4 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CCL20
EC50:
2.9 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CCL21
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CCL1
EC50:
23 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
mouse CCL25
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CCL27
EC50:
37 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CXCL6
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CXCL6
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CXCL11
EC50:
5.1 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CXCL13
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CXCL16
EC50:
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
CX3CL1
EC50:
4.7 nM