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Development of a Triazole Class of Highly Potent Porcn Inhibitors

Development of a Triazole Class of Highly Potent Porcn Inhibitors

Lin You, Chengwei Zhang, Nageswari Yarravarapu, Lorraine Morlock, Xiaolei Wang, Lishu Zhang, Noelle S Williams, Lawrence Lum, Chuo Chen

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5891-5895.

PMID: 27876319

Abstract:

The acyltransferase Porcupine (Porcn) is essential for the secretion of Wnt proteins which contribute to embryonic development, tissue regeneration, and tumorigenesis. We have previously discovered four molecular scaffolds harboring Porcn-inhibitory activity. Comparison of their structures led to the identification of a general scaffold that can be readily assembled by modular synthesis. We report herein the development of a triazole version of this new class of Porcn inhibitors. This study yielded IWP-O1, a Porcn inhibitor with an EC50 value of 80pM in a cultured cell reporter assay of Wnt signaling. Additionally, IWP-O1 has significantly improved metabolic stability over our previously reported Porcn inhibitors.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP2074607488	IWP-O1		2074607-48-8	Price

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