Relaxin family peptides: structure–activity relationship studies

The human relaxin peptide family consists of seven cystine‐rich peptides, four of which are known to signal through relaxin family peptide receptors, RXFP1–4. As these peptides play a vital role physiologically and in various diseases, they are of considerable importance for drug discovery and devel...

Full description

Saved in:
Bibliographic Details
Published in:British journal of pharmacology 2017-05, Vol.174 (10), p.950-961
Main Authors: Patil, Nitin A, Rosengren, K Johan, Separovic, Frances, Wade, John D, Bathgate, Ross A D, Hossain, Mohammed Akhter
Format: Article
Language:English
Subjects:
Antagonists
Drug discovery
Humans
Insulin
Insulin - chemistry
Models, Molecular
Peptides
Proteins - chemistry
Relaxin
Relaxin - analogs & derivatives
Relaxin - chemistry
Review
Structure-Activity Relationship
Themed Section: Review
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The human relaxin peptide family consists of seven cystine‐rich peptides, four of which are known to signal through relaxin family peptide receptors, RXFP1–4. As these peptides play a vital role physiologically and in various diseases, they are of considerable importance for drug discovery and development. Detailed structure–activity relationship (SAR) studies towards understanding the role of important residues in each of these peptides have been reported over the years and utilized for the design of antagonists and minimized agonist variants. This review summarizes the current knowledge of the SAR of human relaxin 2 (H2 relaxin), human relaxin 3 (H3 relaxin), human insulin‐like peptide 3 (INSL3) and human insulin‐like peptide 5 (INSL5). Linked Articles This article is part of a themed section on Recent Progress in the Understanding of Relaxin Family Peptides and their Receptors. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v174.10/issuetoc
ISSN:0007-1188
1476-5381
DOI:10.1111/bph.13684