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

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On July 4th, the Shanghai Overseas Returned Scholars Association invited the Dutch PhD delegation to visit the Chuansha campus of Shanghai Medicilon Inc. (Medicilon) and held discussions with Medicilon's Founder and CEO, Chunlin Chen, among others.

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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.