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Published on: July 6, 2016
Design and synthesis of an ER-specific fluorescent probe based on carboxylesterase activity with quinone methide
Wataru Hakamata1, Aki Machida, Tadatake Oku
1Department of Chemistry and Life Sciences, College of Bioresource Sciences, Nihon University, 1866 Kameino, Fujisawa-shi, Kanagawa 252-0880, Japan. hakamata.wataru@nihon-u.ac.jp
Abstract:
CEs are important enzymes that catalyze the hydrolysis of prodrugs. In this Letter, we present a new mechanistic ER-specific fluorescent probe 1 based on CE activity. Permeation of 1 into cells and subsequent hydrolytic activation by CEs causes spontaneously quinone methide cleavage, resulting in bright red fluorescence in ER with high specificity. Probe 1 was developed for CE activity imaging and inhibitor screening at the cellular level.

