Reference - Detail
| RRC ID | 38254 |
|---|---|
| Author | Hakamata W, Machida A, Oku T, Nishio T. |
| Title | Design and synthesis of an ER-specific fluorescent probe based on carboxylesterase activity with quinone methide cleavage process. |
| Journal | 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. |
| Volume | 21(11) |
| Pages | 3206-9 |
| Published | 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 |
| Times Cited | 45 |
| WOS Category | BIOCHEMISTRY & MOLECULAR BIOLOGY |
| Resource | |
| Human and Animal Cells | COS-1(RCB0143) |