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2010 ; 1799
(10-12
): 829-39
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Aurora kinase inhibitors as anticancer molecules
#MMPMID20863917
Katayama H
; Sen S
Biochim Biophys Acta
2010[Oct]; 1799
(10-12
): 829-39
PMID20863917
show ga
Aurora kinase family of serine/threonine kinases are important regulators of
mitosis that are frequently over expressed in human cancers and have been
implicated in oncogenic transformation including development of chromosomal
instability in cancer cells. In humans, among the three members of the kinase
family, Aurora-A, -B and -C, only Aurora-A and -B are expressed at detectable
levels in all somatic cells undergoing mitotic cell division and have been
characterized in greater detail for their involvement in cellular pathways
relevant to the development of cancer associated phenotypes. Aurora-A and -B are
being investigated as potential targets for anticancer therapy. Development of
inhibitors against Aurora kinases as anticancer molecules gained attention
because of the facts that aberrant expression of these kinases leads to
chromosomal instability and derangement of multiple tumor suppressor and
oncoprotein regulated pathways. Preclinical studies and early phase I and II
clinical trials of multiple Aurora kinase inhibitors as targeted anticancer drugs
have provided encouraging results. This article discusses functional involvement
of Aurora kinase-A and -B in the regulation of cancer relevant cellular
phenotypes together with findings on some of the better characterized Aurora
kinase inhibitors in modulating the functional interactions of Aurora kinases.
Future possibilities about developing next generation Aurora kinase inhibitors
and their clinical utility as anticancer therapeutic drugs are also discussed.
|Animals
[MESH]
|Antineoplastic Agents/chemistry/pharmacology/*therapeutic use
[MESH]
free
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