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ID: ALA1154494

Journal: Bioorg Med Chem Lett

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

Authors: Yatzeck MM, Lavis LD, Chao TY, Chandran SS, Raines RT.

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.

CiteXplore: 18595692

DOI: 10.1016/j.bmcl.2008.06.015