Tankyrase Inhibitors as Therapeutic Targets for Cancer

Author(s): Ahmed Kamal, Sd. Riyaz, Ajay Kumar Srivastava, Abdul Rahim

Journal Name: Current Topics in Medicinal Chemistry

Volume 14 , Issue 17 , 2014

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Graphical Abstract:


Tankyrase 1 and 2 belonging to the family of poly(ADP-ribosyl)ases play an important role in PARsylation by utilizing NAD+ as a substrate in order to generate ADP-ribose polymers. Tankyrases are involved in a number of cellular functions, that includes telomere homeostasis, mitotic spindle formation, vesicle transport linked to glucose metabolism, Wnt/β-catenin signalling, and viral replication. These roles of tankyrases in disease-relevant cellular processes have made them attractive drug targets. Recently, several inhibitors have been identified as potential clinical leads. The current review covers the progress, mechanism and binding modes of recently known Tankyrase inhibitors and discusses the rational approaches that were used to identify the tankyrase inhibitors.

Keywords: Cancer, glucose metabolism, inhibitors, PARsylation, PARP, tankyrase.

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Article Details

Year: 2014
Published on: 28 September, 2014
Page: [1967 - 1976]
Pages: 10
DOI: 10.2174/1568026614666140929115831
Price: $65

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