Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases

Ying-Nan P. Chen, Matthew J. LaMarche, Ho Man Chan, +50

Nature

Cancer ResearchAllosteric InhibitionSignal TransductionSignaling PathwayMedicine +10

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

Jorge Fortanet, Christine Hiu-Tung Chen, Ying-Nan P. Chen, +33

Journal of Medicinal Chemistry

Allosteric InhibitionDrug TargetShp2 InhibitionEfficacious Phosphatase InhibitorChemical Biology +18

Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer

Matthew J. LaMarche, Michael Acker, Andreea Argintaru, +61

Journal of Medicinal Chemistry

Structural reorganization of SHP2 by oncogenic mutations and implications for oncoprotein resistance to allosteric inhibition

Jonathan R. LaRochelle, Michelle Fodor, Vidyasiri Vemulapalli, +7

Nature Communications

Dual Allosteric Inhibition of SHP2 Phosphatase

Michelle Fodor, Edmund V. Price, Ping Wang, +23

ACS Chemical Biology

6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors

Patrick Sarver, Michael Acker, Jeffrey T. Bagdanoff, +27

Journal of Medicinal Chemistry

Medicinal ChemistryAllosteric Shp2 InhibitorsDrug TargetEfficacious Shp2 InhibitorsBiochemistry +13

Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors

Jeffrey T. Bagdanoff, Zhouliang Chen, Michael Acker, +23

Journal of Medicinal Chemistry

Medicinal ChemistrySignaling PathwayReceptor Tyrosine KinaseCell SignalingProtein Function +14

ERG signaling in prostate cancer is driven through PRMT5-dependent methylation of the Androgen Receptor

Zineb Mounir, Joshua M. Korn, Thomas Westerling, +21

eLife

Structural and Functional Consequences of Three Cancer-Associated Mutations of the Oncogenic Phosphatase SHP2

Jonathan R. LaRochelle, Michelle Fodor, Xiang Xu, +10

Biochemistry

Molecular BiologyPtpn11 VariationsTumor BiologySingle Point MutationsSignaling Pathway +17

Identification of an allosteric benzothiazolopyrimidone inhibitor of the oncogenic protein tyrosine phosphatase SHP2

Jonathan R. LaRochelle, Michelle Fodor, Jana M. Ellegast, +9

Bioorganic & Medicinal Chemistry

BiochemistryMedicineReceptor Tyrosine KinaseMechanism Of ActionPharmacology +3