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Glutathione transferase (GST) is a very important metabolic enzyme that mediates the wide metabolism of endogenous and xenobiotic compounds; it usually has a significant over expression in cancer cells, which is a key reason resulting in drug resistance, and will show an obvious down regulation during liver injury, thus it was also regarded as a vital biomarker in clinical diagnosis. Herein, based on boron-dipyrromethene (BODIPY) dye, a two-photon probe BNPA was designed for the real-time detection of GST activities and fluorescence imaging in both cancer cells and liver tissues. Importantly, BNPA exhibited a high selectivity, ultrahigh imaging resolution and showed a classic Michaelis-Menten kinetics toward GSTs. Furthermore, it was successfully used for monitoring the GST activities in living cells and deep tissues by two-photon imaging, as well as detecting the down regulation of GST activities during α-naphthylisothiocyanate (ANIT) induced liver injury. Our results fully demonstrated that BNPA could serve as a promising tool for evaluating the GST function and the process of cellular GSTs in living systems, and also provided a new approach for studying GST-associated liver diseases, which would be greatly useful for rational drug use and disease diagnosis in clinics.
This article was published in the following journal.
Name: Journal of materials chemistry. B
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A glutathione transferase that catalyzes the conjugation of electrophilic substrates to GLUTATHIONE. This enzyme has been shown to provide cellular protection against redox-mediated damage by FREE RADICALS.
A transferase that catalyzes the addition of aliphatic, aromatic, or heterocyclic FREE RADICALS as well as EPOXIDES and arene oxides to GLUTATHIONE. Addition takes place at the SULFUR. It also catalyzes the reduction of polyol nitrate by glutathione to polyol and nitrite.
Fluorescent probe capable of being conjugated to tissue and proteins. It is used as a label in fluorescent antibody staining procedures as well as protein- and amino acid-binding techniques.
A 4-hydroxylated metabolite of AFLATOXIN B1, one of the MYCOTOXINS from ASPERGILLUS tainted food. It is associated with LIVER damage and cancer resulting from its P450 activation to the epoxide which alkylates DNA. Toxicity depends on the balance of liver enzymes that activate it (CYTOCHROME P-450) and others that detoxify it (GLUTATHIONE S TRANSFERASE) (Pharmac Ther 50.443 1991). Primates & rat are sensitive while mouse and hamster are tolerant (Canc Res 29.236 1969).
Conjugation of exogenous substances with various hydrophilic substituents to form water soluble products that are excretable in URINE. Phase II modifications include GLUTATHIONE; ACYLATION; and AMINATION. Phase II enzymes include GLUTATHIONE TRANSFERASE and GLUCURONOSYLTRANSFERASE. In a sense these reactions detoxify phase I reaction products.
Enzymes are proteins that catalyze (i.e., increase the rates of) chemical reactions. In enzymatic reactions, the molecules at the beginning of the process, called substrates, are converted into different molecules, called products. Almost all chemical re...
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Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...