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 v3 and v5 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 v5 integrin.
Cyclic DGR-peptidomimetic containing a bicyclic reverse turn inducer as a selective αvβ5 integrin ligand / A. Trabocchi, G. Menchi, E. Danieli, D. Potenza, N. Cini, A. Bottoncetti, S. Raspanti, A. Pupi, A. Guarna. - In: AMINO ACIDS. - ISSN 0939-4451. - 38:1(2010), pp. 329-337. [10.1007/s00726-009-0255-6]
Cyclic DGR-peptidomimetic containing a bicyclic reverse turn inducer as a selective αvβ5 integrin ligand
D. Potenza;
2010
Abstract
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 v3 and v5 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 v5 integrin.Pubblicazioni consigliate
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