Duraiswamy, Athisayamani Jeyaraj published the artcileDiscovery and Optimization of a Porcupine Inhibitor, Application In Synthesis of 23351-09-9, the publication is Journal of Medicinal Chemistry (2015), 58(15), 5889-5899, database is CAplus and MEDLINE.
Wnt proteins regulate various cellular functions and serve distinct roles in normal development throughout life. Wnt signaling is dysregulated in various diseases including cancers. Porcupine (PORCN) is a membrane-bound O-acyltransferase that palmitoleates the Wnts and hence is essential for their secretion and function. The inhibition of PORCN could serve as a therapeutic approach for the treatment of a number of Wnt-dependent cancers. Herein, the authors describe the identification of a Wnt secretion inhibitor from cellular high throughput screening. Classical SAR based cellular optimization provided us with a PORCN inhibitor I with nanomolar activity and excellent bioavailability that demonstrated efficacy in a Wnt-driven murine tumor model. Finally, the authors also discovered that enantiomeric PORCN inhibitors show very different activity in the reporter assay, suggesting that such compounds may be useful for mode of action studies on the PORCN O-acyltransferase.
Journal of Medicinal Chemistry published new progress about 23351-09-9. 23351-09-9 belongs to alcohols-buliding-blocks, auxiliary class Pyrrole,Benzene,Alcohol, name is 4-(1H-Pyrrol-1-yl)phenol, and the molecular formula is C10H9NO, Application In Synthesis of 23351-09-9.
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