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A highly sensitive fluorogenic probe for cytochrome P450 activity in live cells.

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)=8.8x10(3)M(-1)s(-1) and K(M)=0.09microM. 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.

SUBMITTER: Yatzeck MM

PROVIDER: S-EPMC2586036 | biostudies-literature | 2008 Nov

REPOSITORIES: biostudies-literature

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A highly sensitive fluorogenic probe for cytochrome P450 activity in live cells.

Yatzeck Melissa M MM Lavis Luke D LD Chao Tzu-Yuan TY Chandran Sunil S SS Raines Ronald T RT

Bioorganic & medicinal chemistry letters 20080610 22

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)=8.8x10(3)M(-1)s(-1) and K(M)=0.09microM. 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 resverat ...[more]

PMID: 18595692

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