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De Novo Design and Synthesis of Cyclic and Linear Peptides to Mimic the Binding Cassette of Human Relaxin
Author(s) -
Hossain Mohammed Akhter,
Bathgate Ross A. D.,
Tregear Geoffery,
Wade John D.
Publication year - 2009
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1111/j.1749-6632.2009.03840.x
Subject(s) - relaxin , chemistry , cyclic peptide , peptide , receptor , stereochemistry , combinatorial chemistry , plasma protein binding , biochemistry
A synthetic cyclic regioselectively addressable functionalized template was used to prepare six analogs that presented the side chains of the key receptor‐binding residues of each of H2 and H3 relaxins and insulin‐like peptide 3. None showed any binding affinity for RXFP1, RXFP2, or RXFP3, indicating that the key residues were either incorrectly oriented or that additional residues are required for receptor binding.