Tankyrase Inhibitors

The Tankyrases (TNKS1/PARP5A and TNKS2/PARP5B) are poly (ADP-ribose) polymerases that catalyze the ADP-ribosylation of target proteins. TNKS' are involved in the regulation of Wnt/β-catenin signaling and have been implicated in the pathology of various forms of cancer.

TNKS1 and TNKS2 consist of ankyrin repeats, a SAM domain, and a catalytic ARTD domain. Substrates bind to TNKS through the ankyrin repeats, whereas the SAM domain mediates TNKS multimerization. The ARTD domain catalyzes the ...