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A highly sensitive fluorogenic probe for cytochrome P450 activity in live cells
Tue, 11/27/2012 - 11:47am — root
| Title | A highly sensitive fluorogenic probe for cytochrome P450 activity in live cells |
| Publication Type | Journal Article |
| Year of Publication | 2008 |
| Authors | Yatzeck, MM, Lavis, LD, Chao, TY, Chandran, SS, Raines, RT |
| Journal | Bioorganic & Medicinal Chemistry Letters |
| Volume | 18 |
| Pagination | 5864-5866 |
| Date Published | Nov |
| Accession Number | ISI:000260966800008 |
| Keywords | assay, Carcinogen, carcinogenesis, Chemistry, Medicinal, Chemistry, Organic, CYP1A1 isozyme, Cytochrome P450, dealkylation, Dioxin, enzyme-activity, epithelial-cells, Fluorogenic, induction, latent fluorophore, metabolism, p450, prodrug, resveratrol, Rhodamine 110, substrate, trimethyl lock |
| Abstract | A derivative of rhodamine 110 has been designed and assessed as a probe for cytochrome P450 activity. This probe is the first to utilize a 'trimethyl lock' that is triggered by cleavage of an ether bond. In vitro, fluorescence was manifested by the CYP1A1 isozyme with k(cat)/K-M = 8.8 x 10(3) M (1) s (1) and K-M = 0.09 mu M. In cellulo, the probe revealed the induction of cytochrome P450 activity by the carcinogen 2,3,7,8-tetrachlorodibenzo-p- dioxin, and its repression by the chemoprotectant resveratrol. (C) 2008 Elsevier Ltd. All rights reserved. |
| Short Title | Bioorg. Med. Chem. Lett. |
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