Crystal structure of the tankyrase inhibitor G007-LK in complex with tankyrase 2 (PDB-code 4HYF), University of Oulu
In collaboration with Inven2, the technology transfer office of the University of Oslo, and Oslo University Hospital, we developed late lead stage novel tankyrase inhibitors for oncology. Aberrant WNT/β-catenin signaling is found in multiple cancers. The recently described role of the WNT/β-catenin pathway in regulating immune cell infiltration in the tumor microenvironment suggests an impact of the pathway on immunotherapy. Hence, WNT-directed therapeutic intervention represents an area of significant developmental focus.
The poly(ADP-ribose) polymerases tankyrases 1 and 2 are central targets in the WNT/β-catenin signaling pathway, regulating turnover of the protein complex that controls β-catenin stability and impacting on the hippo signaling pathway. Several small molecules have been identified that inhibit tankyrase 1 and 2, and we have previously shown the efficacy of tankyrase inhibitors in WNT-dependent adenoma and melanoma models.
This project is open for licensing or partnering opportunities. For partnering, MercachemSyncom will be appointed as business partner. Please contact us for further information.