Cell recognition enhanced enzyme hydrolysis of a model peptide-drug conjugate

A model peptide-drug conjugate designed upon a beta-hairpin peptide with the alpha 4 beta 1 integrin recognition sequence LDV appended to the N-terminus and a fluorescent model drug appended to the C-terminus. This model recognizes and binds to alpha 4 beta 1 expressing cells and displays an enhanced rate of enzyme catalyzed hydrolytic model drug release in the presence of the cells compared to the rate in the absence of cells. The present work suggests that peptide-drug conjugate conformation change due to receptor binding may be a viable approach to targeted drug release. (C) 2009 Elsevier Ltd. All rights reserved.