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dc.contributor.authorKarthigeyan, Dhanasekaran
dc.contributor.authorSurabhi, Sudhevan
dc.contributor.authorMizar, Pushpak
dc.contributor.authorSoumik, Siddhanta
dc.contributor.authorBanerjee, Amrita
dc.contributor.authorSinha, Sarmistha Halder
dc.contributor.authorDasgupta, Dipak
dc.contributor.authorNarayana, Chandrabhas
dc.contributor.authorKundu, Tapas Kumar
dc.date.accessioned2017-01-24T06:20:42Z-
dc.date.available2017-01-24T06:20:42Z-
dc.date.issued2016
dc.identifier.citationKarthigeyan, 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.12728en_US
dc.identifier.citationChemical Biology & Drug Designen_US
dc.identifier.citation87en_US
dc.identifier.citation6en_US
dc.identifier.issn1747-0277
dc.identifier.urihttp://hdl.handle.net/10572/2090-
dc.descriptionRestricted Accessen_US
dc.description.abstractAurora 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.uri1747-0285en_US
dc.description.urihttp://dx.doi.org/10.1111/cbdd.12728en_US
dc.language.isoEnglishen_US
dc.publisherWiley-Blackwellen_US
dc.rights@Wiley-Blackwell, 2016en_US
dc.subjectBiochemistry & Molecular Biologyen_US
dc.subjectPharmacology & Pharmacyen_US
dc.subjectAurora kinaseen_US
dc.subjectnon-ATP analogue inhibitoren_US
dc.subjectPTK66en_US
dc.subjectsurface-enhanced Raman spectroscopyen_US
dc.subjectCrystal-Structureen_US
dc.subjectDiscoveryen_US
dc.titleA Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibitionen_US
dc.typeArticleen_US
Appears in Collections:Research Articles (Chandrabhas N.)
Research Papers (Tapas K. Kundu)

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