Relaxin family peptide receptors in GtoPdb v.2023.1

Alexander I. Agoulnik, Ross A.D. Bathgate, Thomas Dschietzig, Andrew L. Gundlach, Michelle Halls, Craig Smith, Roger Summers
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Abstract

Relaxin family peptide receptors (RXFP, nomenclature as agreed by the NC-IUPHAR Subcommittee on Relaxin family peptide receptors [23, 119]) 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 [260]. relaxin-3 is the ligand for RXFP3 but it also binds to RXFP1 and RXFP4 and has differential affinity for RXFP2 between species [259]. INSL5 is the ligand for RXFP4 but is a weak antagonist of RXFP3. relaxin and INSL3 have multiple complex binding interactions with RXFP1 [267] and RXFP2 [132] 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 [262]. INSL5 and relaxin-3 interact with their receptors using distinct residues in their B-chains for binding, and activation, respectively [321, 152].
松弛素家族肽受体在GtoPdb v.2023.1
松弛素家族肽受体(RXFP,由NC-IUPHAR松弛素家族肽受体小组委员会商定的命名法[231,119])可分为两对,RXFP1/2和RXFP3/4。这些受体的内源性激动剂是与胰岛素结构相关的异二聚肽激素:松弛素-1、松弛素、松弛素-3(也称为INSL7)、胰岛素样肽3 (INSL3)和INSL5。松弛素的物种同源物具有不同的药理作用,松弛素与RXFP1、RXFP2和RXFP3相互作用,而小鼠和大鼠松弛素选择性地结合并激活RXFP1[260]。relaxin-3是RXFP3的配体,但它也与RXFP1和RXFP4结合,并且在不同物种之间对RXFP2具有不同的亲和力[259]。INSL5是RXFP4的配体,但是RXFP3的弱拮抗剂。relaxin和INSL3与RXFP1[267]和RXFP2[132]有多种复杂的结合相互作用,这些相互作用指导受体的n端LDLa模块与连接域一起作为系链配体直接受体信号传导[262]。INSL5和relaxin-3分别通过其b链上不同的残基与受体相互作用以结合和激活[321,152]。
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