Abstract
Cancer is a disease portrayed by the uncontrolled growth of irregular cells. Tankyrase, a member of poly(ADP-ribose)polymerase family, mediates Wnt signal transduction and has emerged as a new molecular target for the therapy of different kinds of cancer. Wnt/β-catenin signaling functions significantly in a wide scope of biological events, such as the upkeep of genomic stability, transcriptional control, energy metabolism, and apoptosis. ADP-ribosylation is a reversible posttranslational modification process that regulates several cellular signaling pathways in which transferase enzymes such as mono (ADP-ribosyl) and poly(ADP-ribosyl) transferases move a unit of ADP-ribose moiety from the NAD+ co-substrate to specific amino acid side chains and/or potentially ADP-ribose units on target proteins. Recently, inhibition of tankyrase has risen as an appealing strategy for the discovery of novel anticancer drugs. The current review offers an understanding of the ongoing improvements on new lead structures as inhibitors of tankyrase and their activities. A special spotlight is set on the structure-activity relationship, molecular docking, polypharmacology profile, and binding mode at the active center.
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