期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 10, 页码 4625-4636出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b02001
关键词
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资金
- Cancer Research UK [C309/A8274, C309/A11566]
- NHS
- Cancer Research UK [11566] Funding Source: researchfish
HSP70 is a molecular chaperone and a key component of the heat-shock response. Because of its proposed importance in oncology, this protein has become a popular target for drug discovery, efforts which have as yet brought little success. This study demonstrates that adenosine-derived HSP70 inhibitors potentially bind to the protein with a novel mechanism of action, the stabilization by desolvation of an intramolecular salt-bridge which induces a conformational change in the protein, leading to high affinity ligands. We also demonstrate that through the application of this mechanism, adenosine-derived HSP70 inhibitors can be optimized in a rational manner.
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