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Issue 3, 2014
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Discovery of selective 2,4-diaminopyrimidine-based photoaffinity probes for glyoxalase I

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Abstract

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 selectively bind to GLO-1 in cells. These compounds show potent inhibition of GLO-1 enzyme activity and prevent proliferation of cancer cells. The cell permeable and “clickable” photoaffinity probe L1-Bpyne presented here could be a valuable tool for profiling GLO-1 in live cells.

Graphical abstract: Discovery of selective 2,4-diaminopyrimidine-based photoaffinity probes for glyoxalase I

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Publication details

The article was received on 30 Sep 2013, accepted on 20 Dec 2013 and first published on 06 Feb 2014


Article type: Concise Article
DOI: 10.1039/C3MD00286A
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Citation: Med. Chem. Commun., 2014,5, 352-357
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    Discovery of selective 2,4-diaminopyrimidine-based photoaffinity probes for glyoxalase I

    Y. Zhou, T. Guo, X. Li, Y. Dong, P. Galatsis, D. S. Johnson and Z. Pan, Med. Chem. Commun., 2014, 5, 352
    DOI: 10.1039/C3MD00286A

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