The relaxin receptor as a therapeutic target – perspectives from evolution and drug targeting

RAD Bathgate; M Kocan; DJ Scott; MA Hossain; SV Good; S Yegorov; J Bogerd; PR Gooley

Journal article

The relaxin receptor as a therapeutic target – perspectives from evolution and drug targeting

RAD Bathgate, M Kocan, DJ Scott, MA Hossain, SV Good, S Yegorov, J Bogerd, PR Gooley

Pharmacology and Therapeutics | PERGAMON-ELSEVIER SCIENCE LTD | Published : 2018

DOI: 10.1016/j.pharmthera.2018.02.008

Abstract

The peptide relaxin was first identified as an important circulating hormone during pregnancy over 90 years ago. Research over many years defined the numerous biological roles that relaxin plays throughout pregnancy in many mammalian species. These important biological actions have led to the testing of relaxin as a therapeutic agent for a number of indications. The discovery of the relaxin receptor, RXFP1, in 2002 facilitated the better understanding of the cellular targets of relaxin, its mechanism of action and enabled the development of relaxin mimetics and screening for small molecule agonists. Additionally, the rapid expansion of the genome databases and bioinformatics tools has signif..

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University of Melbourne Researchers

Ross Bathgate Author

Daniel Scott Author

Akhter Hossain Author

Paul Gooley Author

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Grants

Awarded by National Health and Medical Research Council

Funding Acknowledgements

Research described in this review was supported by National Health and Medical Research Council of Australia project grants [628427] and [1043750] (RADB, DJS and PRG) and [1122170] (MAH, RADB, MK) the Victorian Government Operational Infrastructure Support Program and equipment grants from the Australian Research Council [LE120100022]. RADB is supported by an NHMRC Research Fellowship [1042650]. DJS is an NHMRC Boosting Dementia Research Leadership Fellow. SVG is supported by Natural Sciences and Engineering Research Council of Canada (NSERC). JB is supported by the Norwegian Research Council BIOTEK2021 project SALMOSTERILE (221648). The authors would like to thank Daniel Ocampo Daza for the line-drawing animal illustrations used in Figs. 4 and 5.