Synthetic short-chain peptide analogues of H1 relaxin lack affinity for the RXFP1 receptor and relaxin-like bioactivity. Clues to a better understanding of relaxin agonist design

Synthetic short-chain peptide analogues of H1 relaxin lack affinity for the RXFP1 receptor and relaxin-like bioactivity. Clues to a better understanding of relaxin agonist design

The peptide hormone relaxin (RLX), also available as clinical-grade recombinant protein (serelaxin), holds great promise as a cardiovascular and anti-fibrotic agent but is limited by the pharmacokinetic issues common to all peptide drugs. In this study, by a computational modelling chemistry approac...

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Bibliographic Details
Main Authors: Annunziata D'Ercole, Silvia Nistri, Lorenzo Pacini, Alfonso Carotenuto, Federica Santoro, Anna Maria Papini, Ross A. D. Bathgate, Daniele Bani, Paolo Rovero
Format: Article
Language:English
Published: Frontiers Media S.A. 2022-08-01
Series:Frontiers in Pharmacology
Subjects:
relaxin
RXFP1
relaxin analogues
cAMP
ERK1/2
RXFP1 agonists
Online Access:https://www.frontiersin.org/articles/10.3389/fphar.2022.942178/full

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https://www.frontiersin.org/articles/10.3389/fphar.2022.942178/full

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