RRC ID 38254
著者 Hakamata W, Machida A, Oku T, Nishio T.
タイトル Design and synthesis of an ER-specific fluorescent probe based on carboxylesterase activity with quinone methide cleavage process.
ジャーナル Bioorg Med Chem Lett
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.
巻・号 21(11)
ページ 3206-9
公開日 2011-6-1
DOI 10.1016/j.bmcl.2011.04.066
PII S0960-894X(11)00525-7
PMID 21549595
MeSH Animals COS Cells Carboxylesterase / chemistry* Carboxylesterase / metabolism Chlorocebus aethiops Drug Design* Endoplasmic Reticulum / chemistry* Endoplasmic Reticulum / metabolism Fluorescent Dyes / chemical synthesis* Fluorescent Dyes / chemistry Indolequinones / chemistry* Indolequinones / metabolism Molecular Structure
IF 2.74
引用数 45
WOS 分野 BIOCHEMISTRY & MOLECULAR BIOLOGY
リソース情報
ヒト・動物細胞 COS-1(RCB0143)