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.