180854-12-0Relevant articles and documents
An Excimer Clamp for Measuring Damaged-Base Excision by the DNA Repair Enzyme NTH1
Jun, Yong Woong,Wilson, David L.,Kietrys, Anna M.,Lotsof, Elizabeth R.,Conlon, Savannah G.,David, Sheila S.,Kool, Eric T.
supporting information, p. 7450 - 7455 (2020/03/23)
Direct measurement of DNA repair enzyme activities is important both for the basic study of cellular repair pathways as well as for potential new translational applications in their associated diseases. NTH1, a major glycosylase targeting oxidized pyrimidines, prevents mutations arising from this damage, and the regulation of NTH1 activity is important in resisting oxidative stress and in suppressing tumor formation. Herein, we describe a novel molecular strategy for the direct detection of damaged DNA base excision activity by a ratiometric fluorescence change. This strategy utilizes glycosylase-induced excimer formation of pyrenes, and modified DNA probes, incorporating two pyrene deoxynucleotides and a damaged base, enable the direct, real-time detection of NTH1 activity in vitro and in cellular lysates. The probe design was also applied in screening for potential NTH1 inhibitors, leading to the identification of a new small-molecule inhibitor with sub-micromolar potency.
Concise synthesis of aryl-C-nucleosides by Friedel-Crafts alkylation
Hainke, Sven,Arndt, Sebastian,Seitz, Oliver
, p. 4233 - 4238 (2007/10/03)
A fast and simplified synthesis of 1′,2′-dideoxy-1′- pyrenyl-riboside and several other C-nucleosides is shown. Shelf-stable 1-O-methyl-3,5-di-O-toluoyl-2-deoxyribose is demonstrated to serve as a versatile glycosyl donor in Lewis acid promoted Friedel-Cr
Efficient epimerization of pyrene and other aromatic C-nucleosides with trifluoroacetic acid in dichloromethane
Jiang, Yu Lin,Stivers, James T.
, p. 85 - 88 (2007/10/03)
Trifluoroacetic acid has been found to be an efficient and non-oxidative catalyst for the epimerization of pyrene and other C-nucleosides in dichloromethane at ambient temperature. Aspects of the epimerization mechanism are also elucidated.