Several well known integrin ligands were, for the first time, homogenously evaluated in an in-vitro testing system for their binding affinity to six different RGD-binding integrin subtyptes. A peptidomimetic integrin ligand was optimized and functionalized, a cyclic pentapeptide ligand optimized through a N-methylscan and used for molecular imaging. Different modifications of the guanidine group of arginine in integrin ligands strongly influenced their subtype selectivity profiles. Furthermore, a method for the functionalization via the guanidine group was developed to be used during solid phase peptide synthesis. Using this protocol, CXCR4 ligands could be functionalized almost without influencing the binding affinity. Moreover, the adhesion of human mesenchumal stem cells on titan surfaces coated with CXCR4 ligands was investigated.
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Several well known integrin ligands were, for the first time, homogenously evaluated in an in-vitro testing system for their binding affinity to six different RGD-binding integrin subtyptes. A peptidomimetic integrin ligand was optimized and functionalized, a cyclic pentapeptide ligand optimized through a N-methylscan and used for molecular imaging. Different modifications of the guanidine group of arginine in integrin ligands strongly influenced their subtype selectivity profiles. Furthermore,...
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