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A rational approach for the development of reduced‐size analogues of neuropeptide Y with high affinity to the Y 1 receptor
Author(s) -
Rist Beate,
Wieland Heike A.,
Willim KlausDieter,
BeckSickinger Annette G.
Publication year - 1995
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.310010509
Subject(s) - terminal (telecommunication) , neuropeptide y receptor , receptor , neuropeptide , chemistry , stereochemistry , amino acid , biochemistry , computer science , telecommunications
Four sets of centrally truncated analogues of neuropeptide Y have been synthesized. In each series the N‐terminal part was constant, while the C‐terminal segment was systematically varied in length. The C‐ and N‐terminal parts were linked by 6‐aminohexanoic acid. The affinity to the Y 1 receptor was investigated on human neuroblastoma cells SK‐N‐MC. Significant differences were found between the series of peptides as well as within each set. Remarkably, the affinity did not solely depend on the length of the segment, and with increasing numbers of residues the IC 50 values were not always decreased. With a given N‐terminal segment, only one optimal length of the C‐terminal segment was found, which suggests that it is not the amino acids themselves but their 3D arrangement and orientation that is important for high receptor affinity.