Classification of chemerin receptor 2

Receptor Structure, Pharmacology, and DistributionReceptor Amino Acid Sequences, Pharmacological Parameters, Tissue DistributionReferences
Previous namesGPR1
Structural information7TM
Humans355 aa (UniProt P46091) chr. 2q33.3 (Entrez 2825)
Rats353 aa (UniProt P46090) chr. 9q31 (Entrez 25457)
Mice353 aa (UniProt Q8K087) chr. 1C2 (Entrez 241070)
Functional assaysCHO cells transfected with GPR1Barnea et al., 2008; Kennedy et al., 2016
Endogenous agonistsHuman chemerin(21–157) (pEC50∼9)Barnea et al., 2008; Southern et al., 2013; Kennedy et al., 2016
AgonistsC9 [chemerin(149–157)] (pEC50 = 8.65 ± 0.14)Kennedy et al., 2016
C13 [chemerin(145–157)] (pEC50 = 9.05 ± 0.09)Kennedy et al., 2016
C20 [chemerin(138–157)]Li et al., 2014a
Selective antagonistNone
Radioligands[125I]-C9 (KD = 5.3 nM) (pIC50 = 9.3)Barnea et al., 2008; Kennedy et al., 2016
Human [125I]-chemerin(21–157) (KD = 0.21 nM)De Henau et al., 2016
Transduction mechanismsCoupled to Gi/o proteins: predictedRourke et al., 2015
Receptor distribution
HumansNorthern blot analysis identified the GPR1 gene in the hippocampusMarchese et al., 1994b
RT-PCR showed highest expression of GPR1 mRNA in the adrenal cortex, cardiomyocytes, and superior cervical ganglionWu et al., 2009
Immunohistochemistry confirmed GPR1 expression in smooth muscle cells of the vasculatureKaragiannis et al., 2013; Kennedy et al., 2016
MiceRT-PCR identifed highest GPR1 mRNA expression in white adipose tissue (predominately the stromal vascular fraction), with high levels also detected in skin, brown adipose tissue, skeletal muscle, the brain (particularly the hypothalamus), bladder, esophagus, and ovariesRegard et al., 2008; Takahashi et al., 2011; Rourke et al., 2014; Yang et al., 2016
RatsRT-PCR detected GPR1 mRNA in the male reproductive system, with high levels in the testisLi et al., 2014b
Tissue functionHIV/SIV coreceptor; lipid metabolismEdinger et al., 1997; Shimizu et al., 2009; Rourke et al., 2014
  • aa, Amino acid; chr., chromosome; RT-PCR, reverse-transcription polymerase chain reaction; SIV, simian immunodeficiency virus.