Bisubstrate-Type Chemical Probes Identify GRP94 as a Potential Target of Cytosine-Containing Adenosine Analogs
We synthesized affinity-based chemical probes of cytosine-adenosine bisubstrate analogs and identified several potential targets by proteomic analysis. The validation of the proteomic analysis identified the chemical probe as a specific inhibitor of gluco
Discovery of selective 2,4-diaminopyrimidine-based photoaffinity probes for glyoxalase i
Glyoxalase I (GLO-1) plays a critical role in the detoxification of 2-oxoaldehydes and is highly expressed in cancer cells. Through photo-affinity labelling and affinity pull-down approaches, a series of 2,4-diaminopyrimidine compounds were discovered to
Zhou, Yiqing,Guo, Tianlin,Li, Xitao,Dong, Yi,Galatsis, Paul,Johnson, Douglas S.,Pan, Zhengying
p. 352 - 357
(2014/03/21)
Optimization of activity-based probes for proteomic profiling of histone deacetylase complexes
Histone deacetylases (HDACs) are key enzymatic regulators of the epigenome and serve as promising targets for anticancer therapeutics. Recently, we developed a photoreactive "clickable" probe, SAHA-BPyne, to report on HDAC activity and complex formation i
Salisbury, Cleo M.,Cravatt, Benjamin F.
p. 2184 - 2194
(2008/09/18)
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