Discovery of selective 2,4-diaminopyrimidine-based photoaffinity probes for glyoxalase IElectronic supplementary information (ESI) available: Detailed synthetic procedures, 1H and 13C NMR spectra, HPLC chromatograms for compounds L1, L2, L3, L1-Biotin and L1-Bpyne; detailed procedures for biological assays; mass spectroscopy data for GLO-1. See DOI: 10.1039/c3md00286a
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 com...
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creator | Zhou, Yiqing Guo, Tianlin Li, Xitao Dong, Yi Galatsis, Paul Johnson, Douglas S Pan, Zhengying |
description | 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.
L1-Bpyne
was discovered as a potent inhibitor and cell permeable probe of glyoxalase I. |
doi_str_mv | 10.1039/c3md00286a |
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L1-Bpyne
presented here could be a valuable tool for profiling GLO-1 in live cells.
L1-Bpyne
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L1-Bpyne
presented here could be a valuable tool for profiling GLO-1 in live cells.
L1-Bpyne
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L1-Bpyne
presented here could be a valuable tool for profiling GLO-1 in live cells.
L1-Bpyne
was discovered as a potent inhibitor and cell permeable probe of glyoxalase I.</abstract><doi>10.1039/c3md00286a</doi><tpages>6</tpages></addata></record> |
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title | Discovery of selective 2,4-diaminopyrimidine-based photoaffinity probes for glyoxalase IElectronic supplementary information (ESI) available: Detailed synthetic procedures, 1H and 13C NMR spectra, HPLC chromatograms for compounds L1, L2, L3, L1-Biotin and L1-Bpyne; detailed procedures for biological assays; mass spectroscopy data for GLO-1. See DOI: 10.1039/c3md00286a |
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