Specific small-molecule activator of aurora kinase a induces autophosphorylation in a cell-free system

UNSPECIFIED (2008) Specific small-molecule activator of aurora kinase a induces autophosphorylation in a cell-free system. .

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Abstract

Aurora kinases are essential for chromosomal segregation and cell division and thereby important for maintaining the proper genomic integrity. There are three classes of aurora kinases in humans: A, B, and C. Aurora kinase A is frequently overexpressed in various cancers. The link of the overexpression and tumorigenesis is yet to be understood. By employing virtual screening, we have found that anacardic acid, a pentadecane aliphatic chain containing hydroxylcarboxylic acid, from cashew nut shell liquid could be docked in Aurora kinases A and B. Remarkably, we found that anacardic acid could potently activate the Aurora kinase A mediated phosphorylation of histone H3, but at a similar concentration the activity of aurora kinase B remained unaffected in vitro. Mechanistically, anacardic acid induces the structural changes and also the autophosphorylation of the aurora kinase A to enhance the enzyme activity. This data thus indicate anacardic acid as the first small-molecule activator of Aurora kinase, which could be highly useful for probing the function of hyperactive (overexpressed) Aurora kinase A.

Item Type:	Patent
Additional Information:	PMID: 18215015
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	Manjula P Library Assistant
Date Deposited:	26 Aug 2019 07:37
Last Modified:	16 Jul 2022 05:22
URI:	http://eprints.uni-mysore.ac.in/id/eprint/7036

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