NDLI: Identification of Limonol Derivatives as Heat Shock Protein 90 (Hsp90) Inhibitors through a Multidisciplinary Approach

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Identification of Limonol Derivatives as Heat Shock Protein 90 (Hsp90) Inhibitors through a Multidisciplinary Approach

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Identification of Limonol Derivatives as Heat Shock Protein 90 (Hsp90) Inhibitors through a Multidisciplinary Approach

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Leone, Antonietta Bifulco, Giuseppe Chini, Maria G. Gualtieri, Maria J. Vassallo, Antonio Malafronte, Nicola Dal Piaz, Fabrizio Castellano, Sabrina De Tommasi, Nunziatina Vasaturo, Michele Vaccaro, Maria C. Milite, Ciro
Description	Author Affiliation: Chini MG ( Department of Pharmacy, University of Salerno, Via Giovanni Paoloâ II 132, 84084, Fisciano, Italy.); Malafronte N ( Department of Pharmacy, University of Salerno, Via Giovanni Paoloâ II 132, 84084, Fisciano, Italy.); Vaccaro MC ( Department of Pharmacy, University of Salerno, Via Giovanni Paoloâ II 132, 84084, Fisciano, Italy.); Gualtieri MJ ( Department of Pharmacy, University of Salerno, Via Giovanni Paoloâ II 132, 84084, Fisciano, Italy.); Vassallo A ( Department of Pharmacognosy and Organic Drug, University of Los Andes, Sector Campo de Oro, detrás del IAHULA, 5101, Mérida, Venezuela.); Vasaturo M ( Department of Science, University of Basilicata, Viale dell'Ateneo Lucanoâ 10, 85100, Potenza, Italy.); Castellano S ( Department of Pharmacy, University of Salerno, Via Giovanni Paoloâ II 132, 84084, Fisciano, Italy.); Milite C ( PhD Program in Drug Discovery and Development, University of Salerno, Via Giovanni Paoloâ II 132, 84084, Fisciano, Italy.); Leone A ( Department of Pharmacy, University of Salerno, Via Giovanni Paoloâ II 132, 84084, Fisciano, Italy.); Bifulco G ( Department of Medicine and Surgery, University of Salerno, Via Allende, 84081, Baronissi, Italy.); De Tommasi N ( Department of Pharmacy, University of Salerno, Via Giovanni Paoloâ II 132, 84084, Fisciano, Italy.); Dal Piaz F ( Department of Pharmacy, University of Salerno, Via Giovanni Paoloâ II 132, 84084, Fisciano, Italy.)
Abstract	The identification of inhibitors of Hsp90 is currently a primary goal in the development of more effective drugs for the treatment of various types of multidrug resistant malignancies. In an attempt to identify new small molecules modulating the activity of Hsp90, we screened a small library of tetranortriterpenes. A high-affinity interaction with Hsp90 inducible form was uncovered for eight of these compounds, five of which are described here for the first time. By monitoring the ATPase activity and the citrate synthase thermal induced aggregation, compound 1 (cedrelosin A), 3 (7α-limonylacetate), and 5 (cedrelosin B), containing a limonol moiety, were found to be the most effective in compromising the Hsp90α chaperone activity. Consistent with these findings, the three compounds caused a depletion of c-Raf and pAkt Hsp90 client proteins in HeLa and MCF/7 cell lines. Induced fit docking protocol and molecular dynamics were used to rationalize the structural basis of the biological activity of the limonol derivatives. Taken together, these results point to limonol-derivatives as promising scaffolds for the design of novel Hsp90α inhibitors.
ISSN	09476539
e-ISSN	15213765
Journal	Chemistry - A European Journal
Issue Number	37
Volume Number	22
Language	English
Publisher	Wiley-VCH;ChemPubSoc Europe
Publisher Date	2016-09-05
Publisher Place	Germany
Access Restriction	Open
Subject Keyword	Chemistry
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Catalysis

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