International Union of Basic and Clinical Pharmacology. LXXXIX. Update on the Extended Family of Chemokine Receptors and Introducing a New Nomenclature for Atypical Chemokine Receptors (original) (raw)
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Chemokine receptors (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database
IUPHAR/BPS Guide to Pharmacology CITE, 2020
Chemokine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Chemokine Receptors [431, 430, 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 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 [32].Chemokines in turn can be divided by structure into four subclasses by the number and arrangement of conserved cysteines. CC (also known a...
Chemokine receptors in GtoPdb v.2023.1
IUPHAR/BPS Guide to Pharmacology CITE
Chemokine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Chemokine Receptors [438, 437, 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 know...
Mechanisms of Regulation of the Chemokine-Receptor Network
International journal of molecular sciences, 2017
The interactions of chemokines with their G protein-coupled receptors promote the migration of leukocytes during normal immune function and as a key aspect of the inflammatory response to tissue injury or infection. This review summarizes the major cellular and biochemical mechanisms by which the interactions of chemokines with chemokine receptors are regulated, including: selective and competitive binding interactions; genetic polymorphisms; mRNA splice variation; variation of expression, degradation and localization; down-regulation by atypical (decoy) receptors; interactions with cell-surface glycosaminoglycans; post-translational modifications; oligomerization; alternative signaling responses; and binding to natural or pharmacological inhibitors.
Methods, 1996
overall sequence homology. The chemokines play a role Chemokines are a family of small proteins that are present in in the selective activation and recruitment of a large a variety of inflammatory conditions and have been shown to variety of cell types in inflammation, as has been reactivate and recruit a wide variety of cell types. They bind to viewed extensively in this journal. CXC chemokines a family of seven transmembrane G-protein-coupled receptors. are principally involved in the activation of neutro-Models for the interaction of the chemokines with their receptors phils, but are less important in the activation of other suggest a two-step mechanism. Initially, the main body of the leukocytes, such as monocytes. CC chemokines have chemokine interacts with the outside of the receptor (Site 1), the opposite profile in terms of cellular selectivity and and this interaction directs receptor selectivity. Subsequently, have little or no effect on neutrophils. In addition to the flexible amino-terminus of the chemokine interacts with the this selectivity of response, there is also a high degree receptor core (Site 2) to initiate the signaling response. Mutaof potency in chemokines -the majority bind their regenesis studies of IL-8, the archetypal CXC chemokine, show ceptors at nanomolar concentrations and exhibit their that altering the protein on the third b-sheet can change the physiological responses in the subnanomolar concenreceptor selectivity from that of a CXC chemokine and introduce tration range. Chemokines have been implicated in a CC chemokine activity-confirming the role of this region in variety of clinically important inflammatory diseases. Site 1. Mutagenesis studies of the amino-terminal region of IL-
Chemokine inhibition ‒ why, when, where, which and how?
Biochemical Society Transactions, 2004
Chemokines are small chemoattractant cytokines that control a wide variety of biological and pathological processes, ranging from immunosurveillance to inflammation, and from viral infection to cancer. Genetic and pharmacological studies have shown that chemokines are responsible for the excessive recruitment of leucocytes to inflammatory sites and damaged tissue. In the present paper, we discuss the rationale behind interfering with the chemokine system and introduce various points for therapeutic intervention using either protein-based or small-molecule inhibitors. Unlike other cytokines, chemokines signal via seven-transmembrane GPCRs (G-protein-coupled receptors), which are favoured targets by the pharmaceutical industry, and, as such, they are the first cytokines for which small-molecule-receptor antagonists have been developed. In addition to the high-affinity receptor interaction, chemokines have an in vivo requirement to bind to GAGs (glycosaminoglycans) in order to mediate ...
Selectivity and antagonism of chemokine receptors
Journal of …, 1996
The chemokine superfamily can be subdivided into two groups based on their amino terminat cysteine spacing. The CXC chemokines are primarily involved in neutrophil-mediated inflammation and, so far, two human receptors have been cloned. The CC chemokines tend to be involved in chronic inflammation, and recently we have cloned a fourth leukocyte receptor for this group of ligands. it into an antagonist with nanomolar potency. Taken together, this data suggests a two-site model for receptor activation and for selectivity between CC and CXC chemokines, with an initial receptor contact provided by the main body of the chemokine, and activation provided by the amino terminal region.