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Curr Med Chem. 2017 Jul 27. doi: 10.2174/0929867324666170727120315. [Epub ahead of print]

Allosteric Targeting of Aurora A Kinase Using Small Molecules: A Step Forward Towards Next Generation Medicines?

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School of Pharmaceutical Science and Technology, Tianjin University, 92 Weijin Road, Nankai District, Tianjin-3000072. China.
University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW. United Kingdom.


Aurora A (AurA) kinase is a key mitotic protein essential for carrying out numerous cellular functions. Overexpression or malfunction of this enzyme results in numerous human diseases most notably in cancer. Several small molecule inhibitors targeting the ATP binding site of this enzyme are in various stages of clinical development. However, ATP binding site inhibitors can result in selectivity problems often leading to undesirable off-target effects. Moreover, these drugs are prone to drug resistance problem rendering them unfit for long-term administration. Allosteric inhibition of kinases using small molecules is an alternative strategy to target these enzymes and these could serve as the seeds for next generation medicines and minimize any selectivity problems associated with ATP binding site inhibitors. This review discusses the developments in the non-ATP site binding small molecule inhibitors of AurA and their prospect as future therapeutics and tools for chemical biology.


AURKA; AurA-TPX2 inhibition; Aurora A; TPX2; Type IV inhibitors.; allosteric inhibition; kinase inhibitors; protein-protein interaction

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