Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor

SHP2 is a nonreceptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also purportedly plays an important role in the programmed cell death pathway (PD-1/PD-L1). Because it is an oncoprotein associated wit...

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Veröffentlicht in:	Journal of medicinal chemistry 2016-09, Vol.59 (17), p.7773-7782
Hauptverfasser:	Garcia Fortanet, Jorge, Chen, Christine Hiu-Tung, Chen, Ying-Nan P, Chen, Zhouliang, Deng, Zhan, Firestone, Brant, Fekkes, Peter, Fodor, Michelle, Fortin, Pascal D, Fridrich, Cary, Grunenfelder, Denise, Ho, Samuel, Kang, Zhao B, Karki, Rajesh, Kato, Mitsunori, Keen, Nick, LaBonte, Laura R, Larrow, Jay, Lenoir, Francois, Liu, Gang, Liu, Shumei, Lombardo, Franco, Majumdar, Dyuti, Meyer, Matthew J, Palermo, Mark, Perez, Lawrence, Pu, Minying, Ramsey, Timothy, Sellers, William R, Shultz, Michael D, Stams, Travis, Towler, Christopher, Wang, Ping, Williams, Sarah L, Zhang, Ji-Hu, LaMarche, Matthew J
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES Administration, Oral Allosteric Regulation Allosteric Site amines Animals Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology Cell Line, Tumor conformation Crystallography, X-Ray Drug Design Female Heterografts High-Throughput Screening Assays Humans inhibition inhibitors INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY Male Mice, Inbred C57BL Mice, Nude Models, Molecular Neoplasm Transplantation peptides and proteins Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacokinetics Piperidines - pharmacology Protein Conformation Protein Tyrosine Phosphatase, Non-Receptor Type 11 - antagonists & inhibitors Protein Tyrosine Phosphatase, Non-Receptor Type 11 - chemistry Pyrazines - chemical synthesis Pyrazines - chemistry Pyrazines - pharmacokinetics Pyrazines - pharmacology Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacokinetics Pyrimidines - pharmacology Structure-Activity Relationship
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