Mark Lal, Sean Eddy, Anna Walentinsson, Jeffrey B Hodgin, Pernille B L Hansen, Magnus Althage, Matthias Kretzler
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RXFP1, the relaxin receptor: Lost and found in translation.
Relaxin, historically recognized as a pregnancy hormone, is today characterized as a circulating protein possessing several cardiovascular modulating and anti-fibrotic properties of high clinical interest. Although it has long been recognized that there exists remarkable species diversity regarding the tissue sources and physiological effects of relaxin, there is a considerable gap in our translational understanding of its signal transducing receptor, relaxin family peptide receptor 1 (RXFP1). Here, we review the topic and highlight the striking contrast in RXFP1 tissue expression from rodents to humans, and describe how a renewed focus on RXFP1 target pharmacology is critical to delivering future clinical success in relation to this physiologically important signaling receptor.
期刊介绍:
Drug Discovery Today delivers informed and highly current reviews for the discovery community. The magazine addresses not only the rapid scientific developments in drug discovery associated technologies but also the management, commercial and regulatory issues that increasingly play a part in how R&D is planned, structured and executed.
Features include comment by international experts, news and analysis of important developments, reviews of key scientific and strategic issues, overviews of recent progress in specific therapeutic areas and conference reports.