| http://purl.uniprot.org/citations/18582868 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/18582868 | http://www.w3.org/2000/01/rdf-schema#comment | "Relaxin-3 is a potent agonist for both G-protein coupled receptors (GPCR) RXFP3 (also known as GPCR135) and RXFP4 (also known as GPCR142) while insulin-like peptides 5 (INSL5) is a selective RXFP4 agonist. INSL5 is also a weak (low affinity) RXFP3 antagonist. RXFP3 and RXFP4 share about 50% homology. We have used gain-of-function (RXFP3 --> RXFP4) and loss-of-function (RXFP4 --> RXFP3) chimeras to identify the domains critical for the binding and activation induced by INSL5. Replacing extracellular loop (EL) 1 or EL3 of RXFP3 with the corresponding domains from RXFP4 does not change the RXFP3 pharmacological profile. Exchanging the N-terminus and EL2 of RXFP3 with these of RXFP4 results in a chimeric receptor (CR5) with a high affinity for INSL5. However, in contrast to native RXFP4, INSL5 does not elicit an agonist response from CR5. Conversely, replacing the N-terminus and EL2 of RXFP4 with counterparts from RXFP3 (CR15) results in a chimeric receptor for which relaxin-3 and INSL5 are high and low affinity agonists, respectively. Further mutagenesis studies indicate that transmembrane (TM) domains 2, 3 and 5 of RXFP4 are critical determinants of functional receptor activation by INSL5. Replacement of TM2, 3, and 5 of RXFP3 with equivalent domains from RXFP4 results in a chimeric receptor that can be activated by INSL5. These results suggest that the N-terminus and EL2 domains of RXFP3 and RXFP4 are involved in ligand binding while TM2, 3, and 5 are critical for receptor activation."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.ejphar.2008.05.025"xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/author | "Liu C."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/author | "Yu J."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/author | "Zhu J."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/author | "Bonaventure P."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/author | "Kamme F."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/author | "Kuei C."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/author | "Lovenberg T.W."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/author | "Sutton S."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/author | "Atack J."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/date | "2008"xsd:gYear |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/name | "Eur J Pharmacol"xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/pages | "43-52"xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/title | "Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135)."xsd:string |
| http://purl.uniprot.org/citations/18582868 | http://purl.uniprot.org/core/volume | "590"xsd:string |
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