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Gene Review

RXFP4  -  relaxin/insulin-like family peptide...

Homo sapiens

Synonyms: G-protein coupled receptor 100, G-protein coupled receptor GPCR142, GPCR142, GPR100, Insulin-like peptide INSL5 receptor, ...
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Disease relevance of RXFP4


High impact information on RXFP4

  • In a saturation binding assay, (125)I-INSL5 binds GPCR142 with a K(d) value of 2.5 nM [3].
  • Overall, INSL5 behaves as an agonist for GPCR142 similar to relaxin-3 [3].
  • In functional guanosine (gamma-thio)-triphosphate binding and cAMP accumulation assays, INSL5 potently activates GPCR142 with EC(50) values of 1.3 and 1.2 nM, respectively [3].
  • Analysis of possible receptors related to GPCR135 revealed a single orphan receptor, GPCR142 [4].
  • We evaluated by reverse transcriptase-PCR the expression of GPCR142 mRNA in a variety of human tissues and found expression in brain, kidney, testis, thymus, placenta, prostate, salivary gland, thyroid, and colon [4].

Biological context of RXFP4


Associations of RXFP4 with chemical compounds

  • In addition, INSL5 stimulates Ca(2+) mobilization in HEK293 cells expressing GPCR142 and G alpha(16) [3].
  • Boels and Schaller recently reported bradykinin as a ligand for GPCR142 (also known as GPR100) [5].
  • The nonpeptide B(2) receptor agonist FR190997 (8-[2,6-dichloro-3-[N-methylcarbamoyl)cinnamidoacetyl]-N-methylamino]benzyloxy]-2-methyl-4-(2-pyridylmethoxy)quinoline) did inhibit the forskolin-induced cAMP production (pEC(50) = 7.7) at the hB(2)R, whereas it was not able to exert any effect at the hGPR100 [6].
  • FR190997 and relaxin 3 responses at the hB(2)R and hGPR100, respectively, were not inhibited by Icatibant (1 microM) [6].

Regulatory relationships of RXFP4

  • Surprisingly, GPCR142 was activated by nanomolar concentrations of relaxin-3 but was completely unresponsive to all other known insulin-like peptides [4].

Other interactions of RXFP4


Analytical, diagnostic and therapeutic context of RXFP4


  1. Receptors for relaxin family peptides. Bathgate, R.A., Ivell, R., Sanborn, B.M., Sherwood, O.D., Summers, R.J. Ann. N. Y. Acad. Sci. (2005) [Pubmed]
  2. Identification and characterisation of GPR100 as a novel human G-protein-coupled bradykinin receptor. Boels, K., Schaller, H.C. Br. J. Pharmacol. (2003) [Pubmed]
  3. INSL5 is a high affinity specific agonist for GPCR142 (GPR100). Liu, C., Kuei, C., Sutton, S., Chen, J., Bonaventure, P., Wu, J., Nepomuceno, D., Kamme, F., Tran, D.T., Zhu, J., Wilkinson, T., Bathgate, R., Eriste, E., Sillard, R., Lovenberg, T.W. J. Biol. Chem. (2005) [Pubmed]
  4. Identification of relaxin-3/INSL7 as a ligand for GPCR142. Liu, C., Chen, J., Sutton, S., Roland, B., Kuei, C., Farmer, N., Sillard, R., Lovenberg, T.W. J. Biol. Chem. (2003) [Pubmed]
  5. Pharmacological characterization of relaxin-3/INSL7 receptors GPCR135 and GPCR142 from different mammalian species. Chen, J., Kuei, C., Sutton, S.W., Bonaventure, P., Nepomuceno, D., Eriste, E., Sillard, R., Lovenberg, T.W., Liu, C. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  6. Bradykinin B2 and GPR100 receptors: a paradigm for receptor signal transduction pharmacology. Meini, S., Bellucci, F., Cucchi, P., Giuliani, S., Quartara, L., Giolitti, A., Zappitelli, S., Rotondaro, L., Boels, K., Maggi, C.A. Br. J. Pharmacol. (2004) [Pubmed]
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