Yatzeck Melissa M, Lavis Luke D, Chao Tzu-Yuan, Chandran Sunil S, Raines Ronald T
Department of Chemistry, University of Wisconsin-Madison, 1101 University Avenue, Madison, WI 53706-1322, USA.
Bioorg Med Chem Lett. 2008 Nov 15;18(22):5864-6. doi: 10.1016/j.bmcl.2008.06.015. Epub 2008 Jun 10.
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.
一种罗丹明110衍生物已被设计并评估为细胞色素P450活性的探针。该探针是首个利用由醚键裂解触发的“三甲基锁”的探针。在体外，CYP1A1同工酶表现出荧光，其催化常数与米氏常数之比（k(cat)/K(M)）为8.8×10³M⁻¹s⁻¹，米氏常数（K(M)）为0.09微摩尔。在细胞内，该探针揭示了致癌物2,3,7,8 - 四氯二苯并 - p - 二恶英对细胞色素P450活性的诱导作用，以及化学保护剂白藜芦醇对其的抑制作用。
