Classification of chemerin receptor 1

Receptor Structure, Pharmacology, and DistributionReceptor Amino Acid Sequences, Pharmacological Parameters, Tissue DistributionReferences
Previous NamesCMKLR1, ChemR23, ChemerinR, GPCR27, DEZ, RVER1, TIG2 receptor
Structural information7TM
Humans373 aa (UniProt Q99788) chr. 12q24.1 (Entrez 1240)
Rats371 aa (UniProt O35786) chr. 12q16 (Entrez 60669)
Mice371 aa (UniProt P97468) chr. 5F (Entrez 14747)
Functional assaysCHO cells transfected with CMKLR1Wittamer et al., 2003; Barnea et al., 2008
Chemotaxis migration assaysWittamer et al., 2003; Vermi et al., 2005; Zabel et al., 2005b; Albanesi et al., 2009
In vitro pharmacology using isolated human vesselsKennedy et al., 2016
In vitro pharmacology using isolated rat aortaWatts et al., 2013
Endogenous agonistsHuman chemerin(21–157) (pEC50 = 9.37 ± 0.05)Wittamer et al., 2003
RvE1 (pEC50 = 9.37 ± 0.05)Arita et al., 2005
AgonistsC9 [chemerin(149–157)]Wittamer et al., 2009
C13 [chemerin(145–157)]Wittamer et al., 2003
C15 [chemerin(141–155)]Cash et al., 2008
C19 [chemerin(139–157)]Wittamer et al., 2004
C20 [chemerin(138–157)]Li et al., 2014a
Selective antagonistCCX832 (pIC50 = 8.34 ± 0.04)Watts et al., 2013; Kennedy et al., 2016
Radioligands[125I]-C9 (KD = 4.9 nM)Barnea et al., 2008; Kennedy et al., 2016
Human [125I]-chemerin(21–157) (KD = 0.88 nM)De Henau et al., 2016
Human [125I]Tyr-[Phe149]-chemerin146–157 (KD = 22 nM)Wittamer et al., 2003
[3H]RvE1 (KD = 11.3 ± 5.4)Arita et al., 2005, 2007
Mouse [125I]-chemerin(21–148) (EC50 = 1.6 nM)Zabel et al., 2008; Bondue et al., 2012
Transduction mechanismsCoupled to Gi/o proteinsWittamer et al., 2003; Cash et al., 2008; Kennedy et al., 2016
Receptor distribution
HumansRT-PCR showed highest expression of CMKLR1 mRNA in the skin, adipose tissue, spleen, lymph nodes, and lungWittamer et al., 2003; Roh et al., 2007
Immunostaining and FACS analysis confirmed high expression on dendritic cells, monocytes, and macrophagesWittamer et al., 2003; Vermi et al., 2005; Zabel et al., 2005b; Herová et al., 2015
CMKLR1 protein expression was found on smooth muscle cells of human vessels by immunohistochemistryKostopoulos et al., 2014
MiceRT-PCR showed highest CMKLR1 expression in white adipose tissue and the lungGoralski et al., 2007
CMKLR1 immunoreactivity was identified in adipocytesGoralski et al., 2007
RatsRT-PCR–detected CMKLR1 mRNA were in the reproductive system (testis and ovary)Wang et al., 2012; Li et al., 2014b
Western blot analysis and immunohistochemistry identified CMKLR1 expression in vascular endothelial cells, cardiomyocytes and the smooth muscle, and endothelium of aorta and mesenteric vesselsWatts et al., 2013; Zhao et al., 2013; Zhang et al., 2014
Tissue functionChemotaxis of leukocytes; adipogenesis; antimicrobial agent; vasoconstrictor of saphenous vein and resistance arteriesWittamer et al., 2003; Goralski et al., 2007; Cash et al., 2010; Banas, 2013; Kennedy et al., 2016
  • aa, Amino acid; chr., chromosome; FACS, fluorescence-activated cell sorter; RT-PCR, reverse-transcription polymerase chain reaction.