Activation of Relaxin Family Receptor 1 from different mammalian species by relaxin peptide and small molecule agonist ML290

Activation of Relaxin Family Receptor 1 from different mammalian species by relaxin peptide and small molecule agonist ML290

Relaxin peptide (RLN), which signals through the relaxin family peptide 1 (RXFP1) GPCR receptor, has shown therapeutic effects in an acute heart failure clinical trial. We have identified a small molecule agonist of human RXFP1, ML290; however, it does not activate the mouse receptor. To find a suit...

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Bibliographic Details
Main Authors: Zaohua eHuang, Courtney eMyhr, Ross A.D. Bathgate, Brian eHo, Amaya eBueno, Xin eHu, Jingbo eXiao, Noel eSouthall, Elena eBarnaeva, Irina U Agoulnik, Juan eMarugan, Marc eFerrer, Alexander I Agoulnik
Format: Article
Language:English
Published: Frontiers Media S.A. 2015-08-01
Series:Frontiers in Endocrinology
Subjects:
Relaxin
G protein-coupled receptor
RXFP1
Receptor structure-function
small molecule allosteric agonist
Online Access:http://journal.frontiersin.org/Journal/10.3389/fendo.2015.00128/full

Internet

http://journal.frontiersin.org/Journal/10.3389/fendo.2015.00128/full

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