Please use this identifier to cite or link to this item: http://lib.jncasr.ac.in:8080/jspui/handle/10572/2090
Title: A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition
Authors: Karthigeyan, Dhanasekaran
Surabhi, Sudhevan
Mizar, Pushpak
Soumik, Siddhanta
Banerjee, Amrita
Sinha, Sarmistha Halder
Dasgupta, Dipak
Narayana, Chandrabhas
Kundu, Tapas Kumar
Keywords: Biochemistry & Molecular Biology
Pharmacology & Pharmacy
Aurora kinase
non-ATP analogue inhibitor
PTK66
surface-enhanced Raman spectroscopy
Crystal-Structure
Discovery
Issue Date: 2016
Publisher: Wiley-Blackwell
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
Chemical Biology & Drug Design
87
6
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.
Description: Restricted Access
URI: http://hdl.handle.net/10572/2090
ISSN: 1747-0277
Appears in Collections:Research Articles (Chandrabhas N.)
Research Papers (Tapas K. Kundu)

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