42359-42-2Relevant academic research and scientific papers
Cytochrome oxidase CYP1A1 specific fluorescent probe and its preparation method and application
-
, (2019/10/22)
The invention relates to a cytochrome oxidase CYP1A1 specific fluorescent probe, a preparation method and applications thereof, wherein the specific probe substrate has a 4-hydroxynaphthalimide structure, and can be used for determining the CYP1A1 enzyme activity in a biological system. The CYP1A1 enzyme activity determination process comprises: selecting a 4-hydroxynaphthalimide dechloroethylation reaction as a probe reaction, and determining the activity of the CYP1A1 enzyme in various biological samples by quantitatively detecting the generation amount of the dechloroethylation metabolites per unit time. According to the present invention, the cytochrome oxidase CYP1A1 specific fluorescent probe can be used for the quantitative evaluation of the CYP1A1 enzyme activity in biological samples having different species and different individual sources, and the quantitative determination of the CYP1A1 enzyme activity in animal culture cell culture liquids and cell preparation products from different origins so as to evaluate the drug treatment capacity of the important drug metabolic enzyme CYP1A1; and the probe reaction can further be used for rapidly screening inhibitors and inducers of CYP1A1 in vitro and evaluating the inhibition ability.
Target Enzyme-Activated Two-Photon Fluorescent Probes: A Case Study of CYP3A4 Using a Two-Dimensional Design Strategy
Ning, Jing,Wang, Wei,Ge, Guangbo,Chu, Peng,Long, Feida,Yang, Yongliang,Peng, Yulin,Feng, Lei,Ma, Xiaochi,James, Tony D.
supporting information, p. 9959 - 9963 (2019/06/24)
The rapid development of fluorescent probes for monitoring target enzymes is still a great challenge owing to the lack of efficient ways to optimize a specific fluorophore. Herein, a practical two-dimensional strategy was designed for the development of an isoform-specific probe for CYP3A4, a key cytochrome P450 isoform responsible for the oxidation of most clinical drugs. In first dimension of the design strategy, a potential two-photon fluorescent substrate (NN) for CYP3A4 was effectively selected using ensemble-based virtual screening. In the second dimension, various substituent groups were introduced into NN to optimize the isoform-selectivity and reactivity. Finally, with ideal selectivity and sensitivity, NEN was successfully applied to the real-time detection of CYP3A4 in living cells and zebrafish. These findings suggested that our strategy is practical for developing an isoform-specific probe for a target enzyme.
Naphthalimide-based fluorescent off/on probes for the detection of thiols
Sun, Wei,Li, Wenhua,Li, Jing,Zhang, Jian,Du, Lupei,Li, Minyong
, p. 5363 - 5367 (2012/09/07)
Herein, we report the design and synthesis of two naphthalimide-based fluorescent probes. These probes provided high on/off signal ratios and exhibited good selectivity towards thiols over other analytes. Thus, they were identified as good sensors for the
