Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70

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 inhibitor...

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Veröffentlicht in:	Journal of medicinal chemistry 2016-05, Vol.59 (10), p.4625-4636
Hauptverfasser:	Cheeseman, Matthew D, Westwood, Isaac M, Barbeau, Olivier, Rowlands, Martin, Dobson, Sarah, Jones, Alan M, Jeganathan, Fiona, Burke, Rosemary, Kadi, Nadia, Workman, Paul, Collins, Ian, van Montfort, Rob L. M, Jones, Keith
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine - chemical synthesis Adenosine - chemistry Adenosine - pharmacology Crystallography, X-Ray Dose-Response Relationship, Drug HSP70 Heat-Shock Proteins - antagonists & inhibitors HSP70 Heat-Shock Proteins - metabolism Humans Models, Molecular Molecular Conformation Structure-Activity Relationship
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