Relationship between structure and P-grycoprotein inhibitory activity of dimeric opioid peptides containing the Dmt-Tic pharmacophore

摘要

To develop novel inhibitors of P-glycoprotein (P-gp), we investigated the relationship between structure and P-gp activity of dimeric analogs of the canonical structure [(R)2Xaa-Yaa]2Lys-NH2. We found that [(CH3)2Mle-Tic]2Lys-NH2 or its D-Lys analog was found to possess relatively potent P-gp inhibitory activity in K562/DOX cells.