Please use this identifier to cite or link to this item:
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
surface-enhanced Raman spectroscopy
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
Chemical Biology & Drug Design
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
ISSN: 1747-0277
Appears in Collections:Research Articles (Chandrabhas N.)
Research Papers (Tapas K. Kundu)

Files in This Item:
File Description SizeFormat 
  Restricted Access
1.43 MBAdobe PDFView/Open Request a copy

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.