ChemR23/CMKLR1

ChemR23/CMKLR1 is a G protein-coupled chemerin receptor that mediates calcium mobilization and chemotaxis in immature dendritic cells and macrophages^[1]. Mechanistically, chemerin and resolvin E1 activate ChemR23/CMKLR1 to regulate leukocyte trafficking and inflammation-resolution programs^[2]^[3]. In macrophage biology, ChemR23 is functional on M1 macrophages, where chemerin induces chemotaxis, but it is not surface-expressed on M2 macrophages^[4]. Compared with related chemerin receptors, CMKLR1/Chemerin₁ and GPR1/Chemerin₂ both respond to processed chemerin, whereas CCRL2 binds chemerin without classical signaling, supporting distinct experimental interpretation of receptor isoforms^[5]^[6]. In disease models, ChemR23-dependent chemerin activity suppresses inflammation in lung injury, while synthetic chemerin-derived peptides suppress zymosan-induced peritonitis through ChemR23^[7]^[8]. For experimental applications, the small-molecule antagonist CCX832 selectively blocks CMKLR1, and chemerin-derived peptides or resolvin E1 provide agonist tools for studying CMKLR1-driven immune-cell recruitment, inflammation resolution, and receptor-selective signaling^[6]^[8].

References:

[1]. Wittamer V, et al. Specific recruitment of antigen-presenting cells by chemerin, a novel processed ligand from human inflammatory fluids. J Exp Med. 2003 Oct 6;198(7):977-85. [Content Brief]

[2]. Arita M, et al. Resolvin E1 selectively interacts with leukotriene B4 receptor BLT1 and ChemR23 to regulate inflammation. J Immunol. 2007 Mar 15;178(6):3912-7. [Content Brief]

[3]. Herová M, et al. ChemR23, the receptor for chemerin and resolvin E1, is expressed and functional on M1 but not on M2 macrophages. J Immunol. 2015 Mar 1;194(5):2330-7. [Content Brief]

[4]. De Henau O, et al. Signaling Properties of Chemerin Receptors CMKLR1, GPR1 and CCRL2. PLoS One. 2016 Oct 7;11(10):e0164179. [Content Brief]

[5]. Kennedy AJ, et al. International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin₁) and GPR1 (Chemerin₂) Nomenclature, Pharmacology, and Function. Pharmacol Rev. 2018 Jan;70(1):174-196. [Content Brief]

[6]. Cash JL, et al. Synthetic chemerin-derived peptides suppress inflammation through ChemR23. J Exp Med. 2008 Apr 14;205(4):767-75. [Content Brief]

ChemR23/CMKLR1 Antagonist (1)

ChemR23/CMKLR1 Produits associés (1):

By Type:	Selective (1)

Cat. No.	Nom du produit	Effet	Pureté

HY-174140

VU0514009	Antagonist	99.53%
VU0514009 is a competitive chemokine-like receptor 1 (CMKLR1) antagonist (EC₅₀=2 nM). VU0514009 prevents chemerin-9-induced arrestin recruitment and receptor internalization, significantly reducing Ca²⁺ flux response in HEK293 cells. VU0514009 is promising for research of inflammatory diseases and metabolic syndrome.

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