Targeting tankyrase

Researchers from the University of Oslo and Roche's Genentech Inc. unit have developed several selective inhibitors of tankyrases TNKS and TNKS2, two druggable targets in the otherwise hard-to-hit WNT pathway.^1,2 The University team's lead compound has been licensed to Odin Therapeutics A/S for colorectal cancer.

Excessive signaling by the wingless-type MMTV integration site (WNT) pathway drives cell regeneration in a range of solid tumors, but companies have struggled to find therapeutically tractable targets. The tankyrases-a pair of enzymes that normally work by modifying a range of cellular proteins with ADP-ribose-are the best-validated downstream target for inhibiting WNT signaling, according to Genentech senior scientist in the department of cancer targets Mike Costa, whose team has a project to identify new WNT pathway targets...