Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors |
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| Authors: | van Well Renate M Overkleeft Herman S van der Marel Gijsbert A Bruss Dan Thibault Gaétan de Groot Phillip G van Boom Jacques H Overhand Mark |
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| Affiliation: | Leiden Institute of Chemistry, Gorlaeus Laboratories, Leiden University, PO Box 9502, 2300 RA Leiden, The Netherlands. |
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| Abstract: | The solid-phase synthesis of cyclic RGD peptides containing either one or two furanoid sugar amino acids (SAAs) is reported. Using a cyclization-cleavage approach five peptides were successfully assembled and consecutively tested on their ability to bind to the integrin receptors alpha(v)beta(3) and alpha(IIb)beta(3). The cyclic tetrapeptide c[RGD-SAA] (1) showed the most promising activity in an inhibition assay with an IC(50) of 1.49 microM for the alpha(v)beta(3) receptor and 384 nM for the alpha(IIb)beta(3) receptor. |
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