Discovery of Potent and Selective Benzothiophene Difluoromethyl Phosphonate (DFMP) PTPN2/N1-Dual Inhibitors

Journal of Medicinal Chemistry 2026

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Authors: Xiao Mei Zheng, David A. Candito, James Jewell, Matthew Childers, Shuhei Kawamura, Kaitlyn M. Logan, Ryan D. Otte, Charles See Yeung, Dong Xiao, Ping Liu, Duane E. DeMong, Chunhui Huang
+40 more Sulagna Sanyal, Meredeth A. McGowan, Samuel M. Levi, Sebastian E. Schneider, Xavier Fradera, R.L. Palte, Thomas W. Lyons, Kelsey E. Poremba, J Richard Miller, Xiaomei Chai, Zangwei Xu, Isaac Musisi, My Sam Mansueto, Sriraman Venkataraman, Lily Y. Moy, Minjia Zhang, Yi Yang, Mangeng M. Cheng, Robbie McLeod, Jason Laskey, Minilik H. Angagaw, Dustin M. Smith, Ninad Ramesh Varkhede, Eric S. Muise, Alan Bass, Jason M. Walraven, Amy C. Doty, Hongshi Yu, Barbara A. Rath, Laura Engstrom, H Wang, Nicole E. Follmer, Michael Slavonic, Tobias Ehrenberger, Benjamin Nicholson, W Nicholas Haining, David Jonathan Bennett, Erin F. DiMauro, Michelle R. Machacek, Stuart Shumway
DOI: 10.1021/acs.jmedchem.5c03738
Cited by: 1
References: 80

Abstract

as promising structurally differentiated tool to study PTPN1/N2 inhibition and underscore the importance of SLC19A1 in the transport of DFMPs.

Fields of Study & Subjects

Protein Tyrosine Phosphatases PI3K/AKT/mTOR signaling in cancer Protein Kinase Regulation and GTPase Signaling

Publication details

Journal / source
Journal of Medicinal Chemistry
Publisher
American Chemical Society (ACS)
Volume
69
Issue
9
Pages
10515–10530
Publication date
29 April 2026
Language
EN