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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
A chemical-biological study reveals C
9
-type iridoids as novel heat shock protein 90 (Hsp90) inhibitors
Journal of Medicinal Chemistry, Volume 56, No. 4, Year 2013
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Description
The potential of heat shock protein 90 (Hsp90) as a therapeutic target for numerous diseases has made the identification and optimization of novel Hsp90 inhibitors an emerging therapeutic strategy. A surface plasmon resonance (SPR) approach was adopted to screen some iridoids for their Hsp90 α binding capability. Twenty-four iridoid derivatives, including 13 new natural compounds, were isolated from the leaves of Tabebuia argentea and petioles of Catalpa bignonioides. Their structures were elucidated by NMR, electrospray ionization mass spectrometry, and chemical methods. By means of a panel of chemical and biological approaches, four iridoids were demonstrated to bind Hsp90 α. In particular, the dimeric iridoid argenteoside A was shown to efficiently inhibit the chaperone in biochemical and cellular assays. Our results disclose C 9-type iridoids as a novel class of Hsp90 inhibitors. © 2013 American Chemical Society.
Authors & Co-Authors
Dal Piaz, Fabrizio
Italy, Salerno
Università Degli Studi Di Salerno
Vassallo, Antonio
Italy, Potenza
Università Degli Studi Della Basilicata
Temraz, Abeer
Egypt, Cairo
Faculty of Pharmacy
Cotugno, Roberta
Italy, Salerno
Università Degli Studi Di Salerno
Belisario, Maria Antonietta
Italy, Salerno
Università Degli Studi Di Salerno
Bifulco, Giuseppe
Italy, Salerno
Università Degli Studi Di Salerno
Chini, Maria Giovanna
Italy, Salerno
Università Degli Studi Di Salerno
Pisano, Claudio C.P.
Italy, Pomezia
Sigma-tau S.p.a.
De Tommasi, Nunziatina
Italy, Salerno
Università Degli Studi Di Salerno
Braca, Alessandra
Italy, Pisa
Università Di Pisa
Statistics
Citations: 52
Authors: 10
Affiliations: 5
Identifiers
Doi:
10.1021/jm301398y
ISSN:
00222623
e-ISSN:
15204804