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Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors

Discovery of Pyridinyl Acetamide Derivatives as Potent, Selective, and Orally Bioavailable Porcupine Inhibitors

Dai Cheng, Jun Liu, Dong Han, Guobao Zhang, Wenqi Gao, Mindy H Hsieh, Nicholas Ng, Shailaja Kasibhatla, Celin Tompkins, Jie Li, Auzon Steffy, Fangxian Sun, Chun Li, H Martin Seidel, Jennifer L Harris, Shifeng Pan

ACS Med Chem Lett. 2016 May 10;7(7):676-80.

PMID: 27437076

Abstract:

Blockade of aberrant Wnt signaling is an attractive therapeutic approach in multiple cancers. We developed and performed a cellular high-throughput screen for inhibitors of Wnt secretion and pathway activation. A lead structure (GNF-1331) was identified from the screen. Further studies identified the molecular target of GNF-1331 as Porcupine, a membrane bound O-acyl transferase. Structure-activity relationship studies led to the discovery of a novel series of potent and selective Porcupine inhibitors. Compound 19, GNF-6231, demonstrated excellent pathway inhibition and induced robust antitumor efficacy in a mouse MMTV-WNT1 xenograft tumor model.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP603101220	GNF-1331		603101-22-0	Price

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