Journal article

The Structural and Functional Role of the B-chain C-terminal Arginine in the Relaxin-3 Peptide Antagonist, R3(B Delta 23-27)R/I5

Mohammed Akhter Hossain, Ross AD Bathgate, K Johan Rosengren, Fazel Shabanpoor, Suode Zhang, Feng Lin, Geoffrey W Tregear, John D Wade

Chemical Biology and Drug Design | WILEY | Published : 2009

Abstract

Relaxin-3, a member of the insulin superfamily, is involved in regulating stress and feeding behavior. It is highly expressed in the brain and is the endogenous ligand for the receptor RXFP3. As relaxin-3 also interacts with the relaxin receptor RXFP1, selective agonists and antagonists are crucial for studying the physiological function(s) of the relaxin-3/RXFP3 pair. The analog R3(BDelta23-27)R/I5, in which a C-terminally truncated human relaxin-3 (H3) B-chain is combined with the INSL5 A-chain, is a potent selective RXFP3 antagonist and has an Arg residue remaining on the B-chain C-terminus as a consequence of the recombinant protein production process. To investigate the role of this res..

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