Author/Authors :
Renate M. van Well، نويسنده , , Herman S. Overkleeft، نويسنده , , Gijsbert A. van der Marel، نويسنده , , Dan Bruss، نويسنده , , Gaétan Thibault، نويسنده , , Phillip G. de Groot، نويسنده , , Jacques H. van Boom، نويسنده , , Mark Overhand، نويسنده ,
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 αvβ3 and αIIbβ3. The cyclic tetrapeptide c[RGD-SAA] (1) showed the most promising activity in an inhibition assay with an IC50 of 1.49 μM for the αvβ3 receptor and 384 nM for the αIIbβ3 receptor.
