A SMALL LIBRARY OF PEPTIDOMIMETICS TO SYSTEMATICALLY VARY AND TEST THE EFFECTS OF X(1) CONSTRAINTS

Citation
K. Burgess et al., A SMALL LIBRARY OF PEPTIDOMIMETICS TO SYSTEMATICALLY VARY AND TEST THE EFFECTS OF X(1) CONSTRAINTS, Bioorganic & medicinal chemistry letters, 6(22), 1996, pp. 2761-2764
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
6
Issue
22
Year of publication
1996
Pages
2761 - 2764
Database
ISI
SICI code
0960-894X(1996)6:22<2761:ASLOPT>2.0.ZU;2-S
Abstract
A library of 47 peptidomimetics of YGGFLRFa was prepared wherein 32 of these contained 2,3-methanoleucine. This library was tested for bindi ng the neuropeptide FF receptor where neuropeptide FF is FLFQPQRFa, an anti-opiate peptide. This study illustrates how conformational constr aints can be systematically varied in a library format to determine th e best conformational restrictions for the desired activity. Copyright (C) 1996 Elsevier Science Ltd