Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors [electronic resource]

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Tác giả:

Ngôn ngữ: eng

Ký hiệu phân loại: 547.2 Organic chemical reactions formerly 547.139

Thông tin xuất bản: Washington, D.C. : Oak Ridge, Tenn. : United States. Dept. of Energy. Office of Science ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2015

Mô tả vật lý: Size: p. 217-222 : , digital, PDF file.

Bộ sưu tập: Metadata

ID: 261081

 A novel series of potent and selective hexokinase 2 (HK2) inhibitors, 2,6-disubstituted glucosamines, has been identified based on HTS hits, exemplified by compound 1. Inhibitor-bound crystal structures revealed that the HK2 enzyme could adopt an ?induced-fit? conformation. The SAR study led to the identification of potent HK2 inhibitors, such as compound 34 with greater than 100-fold selectivity over HK1. Compound 25 inhibits in situ glycolysis in a UM-UC-3 bladder tumor cell line via <
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 CNMR measurement of [3-<
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 C]lactate produced from [1,6-<
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 ]glucose added to the cell culture.
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