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.
Current Topics in Medicinal Chemistry
Title:Tankyrase Inhibitors as Therapeutic Targets for Cancer
Volume: 14 Issue: 17
Author(s): Ahmed Kamal, Sd. Riyaz, Ajay Kumar Srivastava and Abdul Rahim
Affiliation:
Keywords: Cancer, glucose metabolism, inhibitors, PARsylation, PARP, tankyrase.
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.
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Cite this article as:
Kamal Ahmed, Riyaz Sd., Srivastava Kumar Ajay and Rahim Abdul, Tankyrase Inhibitors as Therapeutic Targets for Cancer, Current Topics in Medicinal Chemistry 2014; 14 (17) . https://dx.doi.org/10.2174/1568026614666140929115831
DOI https://dx.doi.org/10.2174/1568026614666140929115831 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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