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Anticancer Agents Med Chem. 2019 Oct 19. doi: 10.2174/1871520619666191019114321. [Epub ahead of print]

Zoning in on Tankyrases: A Brief Review on the Past, Present and Prospective Studies.

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Molecular Bio-computation and Drug Design Laboratory, School of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4001. South Africa.



Tankyrases are known for their multifunctionalities within the poly(ADPribose) polymerases family and play vital roles in various cellular processes which includes the regulation of tumour suppressors. Tankyrases, which exists in two isoforms; Tankyrase 1 and 2, are highly homologous and are an integral part of the Wnt β-catenin pathway that becomes overly dysregulated when hijacked by pro-carcinogenic machineries. Objective/ Methods: In this review, we cover the distinct roles of the Tankyrase isoforms and their involvement in disease pathogenesis. Also, we provide updates on experimentally and computationally derived antagonists of Tankyrase whilst highlighting the precedence of integrative computer-aided drug design methods towards the discovery of selective inhibitors.


Despite the high prospects embedded in the therapeutic targeting and blockade of Tankyrase isoforms, the inability of small molecule inhibitors to achieve selective targeting has remained a major setback, even until date. This explains numerous incessant drug design efforts geared towards the development of highly selective inhibitors of the respective Tankyrase isoforms since they mediate distinct aberrancies in disease progression. Therefore, considering the setbacks of conventional drug design methods, can computer-aided approaches actually save the day.


The implementation of computer-aided drug design techniques in Tankyrase research could help complement experimental methods and facilitate ligand/structure-based design and discovery of small molecule inhibitors with enhanced selectivity.


Tankyrase; cancer therapy; computer-aided drug design; inhibitors; selective targeting; structural homology

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