Jo Waaler

Discovery of Tankyrase scaffolding inhibitor specifically targeting the ARC4 peptide binding domain

The paper identifies a Tankyrase scaffolding inhibitor, S8 (ARCher-142), that selectively targets the ARC4 peptide binding domain with 8 µM potency.

Tankyrase inhibition demonstrates anti-fibrotic effects in preclinical pulmonary fibrosis models

This study shows that the TNKS inhibitor OM-153 reduces fibrosis markers and ECM expression in multiple preclinical IPF models by inhibiting WNT/β-catenin and YAP signaling.

Substitutions at the C-8 position of quinazolin-4-ones improve the potency of nicotinamide site binding tankyrase inhibitors

This study identifies C-8 position substitutions in quinazolin-4-ones that enhance the potency and selectivity of tankyrase inhibitors by improving interactions with TNKS2.