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ID: ALA1777747

Journal: Bioorg Med Chem Lett

Title: Design and synthesis of an ER-specific fluorescent probe based on carboxylesterase activity with quinone methide cleavage process.

Authors: Hakamata W, Machida A, Oku T, Nishio T.

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.

CiteXplore: 21549595

DOI: 10.1016/j.bmcl.2011.04.066