International Union of Basic and Clinical Pharmacology. XCV. Recent Advances in the Understanding of the Pharmacology and Biological Roles of Relaxin Family Peptide Receptors 1-4, the Receptors for Relaxin Family Peptides

Michelle L Halls; Ross AD Bathgate; Steve W Sutton; Thomas B Dschietzig; Roger J Summers

Journal article

International Union of Basic and Clinical Pharmacology. XCV. Recent Advances in the Understanding of the Pharmacology and Biological Roles of Relaxin Family Peptide Receptors 1-4, the Receptors for Relaxin Family Peptides

Michelle L Halls, Ross AD Bathgate, Steve W Sutton, Thomas B Dschietzig, Roger J Summers

PHARMACOLOGICAL REVIEWS | AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS | Published : 2015

DOI: 10.1124/pr.114.009472

Abstract

Relaxin, insulin-like peptide 3 (INSL3), relaxin-3, and INSL5 are the cognate ligands for the relaxin family peptide (RXFP) receptors 1-4, respectively. RXFP1 activates pleiotropic signaling pathways including the signalosome protein complex that facilitates high-sensitivity signaling; coupling to Gα(s), Gα(i), and Gα(o) proteins; interaction with glucocorticoid receptors; and the formation of hetero-oligomers with distinctive pharmacological properties. In addition to relaxin-related ligands, RXFP1 is activated by Clq-tumor necrosis factor-related protein 8 and by small-molecular-weight agonists, such as ML290 [2-isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide],..

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University of Melbourne Researchers

Ross Bathgate Author Florey Department of Neuroscience and Mental Health

Related Projects (2)

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Grants

Awarded by National Health and Medical Research Council (NHMRC) of Australia

Awarded by RD Wright Career Development Fellowship

Awarded by NHMRC

Awarded by BAS Medical Inc.

Awarded by Zentrales Innovationsprogramm Mittelstand

Awarded by Wellcome Trust

Funding Acknowledgements

M.L.H. was supported by the National Health and Medical Research Council (NHMRC) of Australia Project Grant 1047633 and RD Wright Career Development Fellowship 1061687. R.A.D.B. was supported by NHMRC Project Grants 628427 and 1043750, by the Victorian Government Operational Infrastructure Support Program, and by a NHMRC Research Fellowship. R.J.S. was supported by NHMRC Program Grants 519461 and 1055134. T.B.D. was supported by Grants 89874634 and 89844575 from BAS Medical Inc. and Grants KF2181501AJ9 and KF2318301 from Zentrales Innovationsprogramm Mittelstand. NC-IUPHAR is supported in part by Wellcome Trust Grant 099156/Z/12/Z.