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- Title
Design of Allosteric Stimulators of the Hsp90 ATPase as New Anticancer Leads.
- Authors
D'Annessa, Ilda; Sattin, Sara; Tao, Jiahui; Pennati, Marzia; Sànchez ‐ Martìn, Carlos; Moroni, Elisabetta; Rasola, Andrea; Zaffaroni, Nadia; Agard, David A.; Bernardi, Anna; Colombo, Giorgio
- Abstract
Allosteric compounds that stimulate Hsp90 adenosine triphosphatase (ATPase) activity were rationally designed, showing anticancer potencies in the low micromolar to nanomolar range. In parallel, the mode of action of these compounds was clarified and a quantitative model that links the dynamic ligand-protein cross-talk to observed cellular and in vitro activities was developed. The results support the potential of using dynamics-based approaches to develop original mechanism-based cancer therapeutics.
- Subjects
ALLOSTERIC proteins; ALLOSTERIC regulation; ADENOSINE triphosphatase; ANTINEOPLASTIC agents; PROTEIN-ligand interactions
- Publication
Chemistry - A European Journal, 2017, Vol 23, Issue 22, p5188
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201700169