Conjugates of modified cryptophycins and RGD-peptides enter target cells by endocytosis

…, B Sammet, R Palmisano, S Royo Gracia…

Index: Nahrwold, Markus; Weiss, Christine; Bogner, Tobias; Mertink, Felix; Conradi, Jens; Sammet, Benedikt; Palmisano, Ralf; Royo Gracia, Soledad; Preusse, Thomas; Sewald, Norbert Journal of Medicinal Chemistry, 2013 , vol. 56, # 5 p. 1853 - 1864

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Citation Number: 17

Abstract

Tumor targeting anticancer drug conjugates that contain a tumor recognition motif (homing device) are of high current relevance. Cryptophycins, naturally occurring cytotoxic cyclo- depsipeptides, have been modified by total synthesis to provide analogues suitable for conjugation to peptide-based homing devices. An array of functionalized β2-amino acids was synthesized and incorporated into cryptophycins. All analogues proved to be highly ...