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A rational approach for the development of reduced-size analogues of neuropeptide Y with high affinity to the Y1 receptor

✍ Scribed by Beate Rist; Heike A. Wieland; Klaus-Dieter Willim; Dr Annette G. Beck-Sickinger

Publisher
John Wiley and Sons
Year
1995
Tongue
English
Weight
662 KB
Volume
1
Category
Article
ISSN
1075-2617

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✦ Synopsis

Abstract

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.

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✍ Denise Zwanziger; Ilka Böhme; Diana Lindner; Annette G. Beck-Sickinger 📂 Article 📅 2009 🏛 John Wiley and Sons 🌐 English ⚖ 368 KB

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