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Tankyrase 1/2 impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer

2023-07-11

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Tankyrase 1 and 2 (TNKS1/2) impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer. OM-153 shows picomolar IC₅₀ inhibition in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable ADME properties, and an improved pharmacokinetic profile in mice. The pharmacokinetic analyses in mice were performed according to the standard protocols of Medicilon.

Reference:

Ruben G G Leenders, et al. Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II. J Med Chem. 2021 Dec 23;64(24):17936-17949. doi: 10.1021/acs.jmedchem.1c01264.

Tankyrase WNT Hippo signaling-pathway ADME pharmacokinetic

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