IUPHAR/BPS Guide to Pharmacology CITE
https://doi.org/10.2218/gtopdb/F60/2019.4

Relaxin family peptide receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database



Ross Bathgate1, Thomas Dschietzig2, Andrew L. Gundlach1, Michelle Halls3 and Roger Summers3
  1. University of Melbourne, Australia
  2. Charité-University Medicine Berlin, Germany
  3. Monash University, Australia


Abstract

Relaxin family peptide receptors (RXFP, nomenclature as agreed by the NC-IUPHAR Subcommittee on Relaxin family peptide receptors [18, 75]) may be divided into two pairs, RXFP1/2 and RXFP3/4. Endogenous agonists at these receptors are heterodimeric peptide hormones structurally related to insulin: relaxin-1, relaxin, relaxin-3 (also known as INSL7), insulin-like peptide 3 (INSL3) and INSL5. Species homologues of relaxin have distinct pharmacology and relaxin interacts with RXFP1, RXFP2 and RXFP3, whereas mouse and rat relaxin selectively bind to and activate RXFP1 [172]. relaxin-3 is the ligand for RXFP3 but it also binds to RXFP1 and RXFP4 and has differential affinity for RXFP2 between species [170]. INSL5 is the ligand for RXFP4 but is a weak antagonist of RXFP3. relaxin and INSL3 have multiple complex binding interactions with RXFP1 [176] and RXFP2 [84] which direct the N-terminal LDLa modules of the receptors together with a linker domain to act as a tethered ligand to direct receptor signaling [173]. INSL5 and relaxin-3 interact with their receptors using distinct residues in their B-chains for binding, and activation, respectively [211, 97].

Contents

This is a citation summary for Relaxin family peptide receptors in the Guide to Pharmacology database (GtoPdb). It exists purely as an adjunct to the database to facilitate the recognition of citations to and from the database by citation analyzers. Readers will almost certainly want to visit the relevant sections of the database which are given here under database links.

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Database links

Relaxin family peptide receptors
http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=60
Introduction to Relaxin family peptide receptors
http://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=60
    Receptors
            RXFP1
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=351
            RXFP2
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=352
            RXFP3
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=353
            RXFP4
            http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=354

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