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Article Publish Status: FREE
Abstract Title:

The anti-tumor diterpene oridonin is a direct inhibitor of Nucleolin in cancer cells.

Abstract Source:

Sci Rep. 2018 11 13 ;8(1):16735. Epub 2018 Nov 13. PMID: 30425290

Abstract Author(s):

Michele Vasaturo, Roberta Cotugno, Lorenzo Fiengo, Claudio Vinegoni, Fabrizio Dal Piaz, Nunziatina De Tommasi

Article Affiliation:

Michele Vasaturo

Abstract:

The bioactive plant diterpene oridonin displays important pharmacological activities and is widely used in traditional Chinese medicine; however, its molecular mechanism of action is still incompletely described. In vitro and in vivo data have demonstrated anti-tumor activity of oridonin and its ability to interfere with several cell pathways; however, presently only the molecular chaperone HSP70 has been identified as a direct potential target of this compound. Here, using a combination of different proteomic approaches, innovative Cellular Thermal Shift Assay (CETSA) experiments, and classical biochemical methods, we demonstrate that oridonin interacts with Nucleolin, effectively modulating the activity of this multifunctional protein. The ability of oridonin to target Nucleolin and/or HSP70 could account for the bioactivity profile of this plant diterpene. Recently, Nucleolin has attracted attention as a druggable target, as its diverse functions are implicated in pathological processes such as cancer, inflammation, and viral infection. However, up to now, no small molecule as Nucleolin binders has been reported, thus our finding represents the first evidence of Nucleolin modulation by a small inhibitor.

Study Type : In Vitro Study
Additional Links
Pharmacological Actions : Chemotherapeutic : CK(2328) : AC(1407)

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