Nomenclature for the chemerin receptors is presented as recommended by NC-IUPHAR [4-5]). The chemoattractant protein and adipokine, chemerin (RARRES2, Q99969), has been shown to be the endogenous ligand for both chemerin family receptors. Chemerin₁ was the founding family member, and when GPR1 was de-orphanised it was re-named Chermerin₂ [5]. Chemerin₁ is also activated by the lipid-derived, anti-inflammatory ligand resolvin E1 (RvE1), which is formed via the sequential metabolism of EPA by aspirin-modified cyclooxygenase and lipoxygenase [1-2]. In addition, two GPCRs for resolvin D1 (RvD1) have been identified: FPR2/ALX, the lipoxin A₄ receptor, and GPR32, an orphan receptor [7].

CCX832 (structure not disclosed) is a selective antagonist, pK_i=9.2 [6].

* Key recommended reading is highlighted with an asterisk

* Kennedy AJ, Davenport AP. (2018) International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin1) and GPR1 (Chemerin2) Nomenclature, Pharmacology, and Function. Pharmacol Rev, 70 (1): 174-196. [PMID:29279348]

* Shin WJ, Zabel BA, Pachynski RK. (2018) Mechanisms and Functions of Chemerin in Cancer: Potential Roles in Therapeutic Intervention. Front Immunol, 9: 2772. [PMID:30555465]

1. Arita M, Bianchini F, Aliberti J, Sher A, Chiang N, Hong S, Yang R, Petasis NA, Serhan CN. (2005) Stereochemical assignment, antiinflammatory properties, and receptor for the omega-3 lipid mediator resolvin E1. J Exp Med, 201 (5): 713-22. [PMID:15753205]

2. Arita M, Ohira T, Sun YP, Elangovan S, Chiang N, Serhan CN. (2007) Resolvin E1 selectively interacts with leukotriene B4 receptor BLT1 and ChemR23 to regulate inflammation. J Immunol, 178 (6): 3912-7. [PMID:17339491]

3. Barnea G, Strapps W, Herrada G, Berman Y, Ong J, Kloss B, Axel R, Lee KJ. (2008) The genetic design of signaling cascades to record receptor activation. Proc Natl Acad Sci USA, 105 (1): 64-9. [PMID:18165312]

4. Davenport AP, Alexander SP, Sharman JL, Pawson AJ, Benson HE, Monaghan AE, Liew WC, Mpamhanga CP, Bonner TI, Neubig RR et al.. (2013) International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. Pharmacol Rev, 65 (3): 967-86. [PMID:23686350]

5. Kennedy AJ, Davenport AP. (2018) International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin1) and GPR1 (Chemerin2) Nomenclature, Pharmacology, and Function. Pharmacol Rev, 70 (1): 174-196. [PMID:29279348]

6. Kennedy AJ, Yang P, Read C, Kuc RE, Yang L, Taylor EJ, Taylor CW, Maguire JJ, Davenport AP. (2016) Chemerin Elicits Potent Constrictor Actions via Chemokine-Like Receptor 1 (CMKLR1), not G-Protein-Coupled Receptor 1 (GPR1), in Human and Rat Vasculature. J Am Heart Assoc, 5 (10). [PMID:27742615]

7. Krishnamoorthy S, Recchiuti A, Chiang N, Yacoubian S, Lee CH, Yang R, Petasis NA, Serhan CN. (2010) Resolvin D1 binds human phagocytes with evidence for proresolving receptors. Proc Natl Acad Sci USA, 107 (4): 1660-5. [PMID:20080636]

8. Shimizu N, Soda Y, Kanbe K, Liu HY, Jinno A, Kitamura T, Hoshino H. (1999) An orphan G protein-coupled receptor, GPR1, acts as a coreceptor to allow replication of human immunodeficiency virus types 1 and 2 in brain-derived cells. J Virol, 73 (6): 5231-9. [PMID:10233994]