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A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition

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dc.contributor.author Karthigeyan, Dhanasekaran
dc.contributor.author Surabhi, Sudhevan
dc.contributor.author Mizar, Pushpak
dc.contributor.author Soumik, Siddhanta
dc.contributor.author Banerjee, Amrita
dc.contributor.author Sinha, Sarmistha Halder
dc.contributor.author Dasgupta, Dipak
dc.contributor.author Narayana, Chandrabhas
dc.contributor.author Kundu, Tapas Kumar
dc.date.accessioned 2017-01-24T06:20:42Z
dc.date.available 2017-01-24T06:20:42Z
dc.date.issued 2016
dc.identifier.citation Karthigeyan, D.; Surabhi, S.; Mizar, P.; Soumik, S.; Banerjee, A.; Sinha, S. H.; Dasgupta, D.; Narayana, C.; Kundu, T. K., A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition. Chemical Biology & Drug Design 2016, 87 (6), 958-967 http://dx.doi.org/10.1111/cbdd.12728 en_US
dc.identifier.citation Chemical Biology & Drug Design en_US
dc.identifier.citation 87 en_US
dc.identifier.citation 6 en_US
dc.identifier.issn 1747-0277
dc.identifier.uri https://libjncir.jncasr.ac.in/xmlui/10572/2090
dc.description Restricted Access en_US
dc.description.abstract Aurora kinases are the most commonly targeted mitotic kinases in the intervention of cancer progression. Here, we report a resorcinol derivative, 5-methyl-4(2-thiazolylazo) resorcinol (PTK66), a dual inhibitor of Aurora A and Aurora B kinases. PTK66 is a surface binding non-ATP analogue inhibitor that shows a mixed pattern of inhibition against both of Aurora A and B kinases. The in vitro IC50 is approximately 47 and 40 mu M for Aurora A and Aurora B kinases, respectively. In cellular systems, PTK66 exhibits a substantially low cytotoxicity at micromolar concentrations but it can induce aneuploidy under similar dosages as a consequence of Aurora kinase inhibition. This result was corroborated by a drop in the histone H3 (S10) phosphorylation level detected via Western blot analysis using three different cell types. Altogether, our findings indicate that the ligand containing resorcinol backbone is one of the novel scaffolds targeting the Aurora family of kinases, which could be a target for antineoplastic drug development. en_US
dc.description.uri 1747-0285 en_US
dc.description.uri http://dx.doi.org/10.1111/cbdd.12728 en_US
dc.language.iso English en_US
dc.publisher Wiley-Blackwell en_US
dc.rights @Wiley-Blackwell, 2016 en_US
dc.subject Biochemistry & Molecular Biology en_US
dc.subject Pharmacology & Pharmacy en_US
dc.subject Aurora kinase en_US
dc.subject non-ATP analogue inhibitor en_US
dc.subject PTK66 en_US
dc.subject surface-enhanced Raman spectroscopy en_US
dc.subject Crystal-Structure en_US
dc.subject Discovery en_US
dc.title A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition en_US
dc.type Article en_US


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