[摘要]：Adamantane scaffolds for affinity maturation of prostate cancer specific ligands of low mol. mass are described. These scaffolds are modular and can be used for conjugation of up to three ligands and an addnl. effector mol. by std. peptide coupling techniques. The potential of the scaffolds is demonstrated with the multimerization of GPI 1, a prostate cancer specific small mol. A detailed study of multimerized GPI conjugates with near-IR fluorophores and their binding properties to different prostate cancer cell lines shows the specific binding of these conjugates to cell types pos. for prostate specific membrane antigen (PSMA). We demonstrate that these conjugates allow the sensitive imaging of prostate cancer cells with NIR methodol. and suggest that our adamantane scaffolds might be generally useful for affinity maturation of small mols. targeting cell surface epitopes.
