期刊
AMINO ACIDS
卷 38, 期 1, 页码 329-337出版社
SPRINGER WIEN
DOI: 10.1007/s00726-009-0255-6
关键词
Amino acids; Peptides; Peptidomimetics; Bicyclic compounds; Conformational analysis
资金
- Universita degli Studi di Firenze
- MIUR
3-Aza-6,8-dioxabicyclo[3.2.1]octane-based amino acids as reverse turn inducers have been introduced into cyclic peptidomimetics containing the RGD or DGR retro-sequence, in order to achieve a stereochemical scanning of the binding capability of the resulting molecules towards alpha(v)beta(3) and alpha(v)beta(5) integrins, resulting in retro-inverso DGR peptides as micromolar ligands. A comparative analysis between the conformational preferences of 4 and of its isomer 3, having the opposite RGD sequence, was reported with respect to the binding activity, giving insight into the factors affecting the preferential binding of 4 to the alpha(v)beta(5) integrin.
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