Skip to main content
U.S. Department of Energy
Office of Scientific and Technical Information

Targeted Degradation of the Oncogenic Phosphatase SHP2

Journal Article · · Biochemistry-US

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; National Institutes of Health (NIH); UNIVERSITY
OSTI ID:
1829853
Journal Information:
Biochemistry-US, Vol. 60, Issue (34)
Country of Publication:
United States
Language:
ENGLISH

References (34)

Activating Mutations of the Noonan Syndrome-Associated SHP2/PTPN11 Gene in Human Solid Tumors and Adult Acute Myelogenous Leukemia journal December 2004
Somatic mutations in PTPN11 in juvenile myelomonocytic leukemia, myelodysplastic syndromes and acute myeloid leukemia journal April 2003
Structural mechanism associated with domain opening in gain-of-function mutations in SHP2 phosphatase: Domain Opening in SHP2 Phosphatase journal March 2011
Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases journal June 2016
PD-1 immunoreceptor inhibits B cell receptor-mediated signaling by recruiting src homology 2-domain-containing tyrosine phosphatase 2 to phosphotyrosine journal November 2001
SHP2 inhibition triggers anti-tumor immunity and synergizes with PD-1 blockade journal March 2019
Combinations with Allosteric SHP2 Inhibitor TNO155 to Block Receptor Tyrosine Kinase Signaling journal October 2020
Structural and Functional Consequences of Three Cancer-Associated Mutations of the Oncogenic Phosphatase SHP2 journal April 2016
Off-target inhibition by active site-targeting SHP2 inhibitors journal August 2018
Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application journal May 2020
Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor journal July 2016
RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers journal August 2018
Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer journal September 2020
A12 The SHP2 Inhibitor RMC-4630 in Patients with KRAS-Mutant Non-Small Cell Lung Cancer: Preliminary Evaluation of a First-in-Man Phase 1 Clinical Trial journal February 2020
Resistance to allosteric SHP2 inhibition in FGFR-driven cancers through rapid feedback activation of FGFR journal January 2020
Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome journal August 2018
XDS journal January 2010
Coot model-building tools for molecular graphics journal November 2004
Towards automated crystallographic structure refinement with phenix.refine journal March 2012
electronic Ligand Builder and Optimization Workbench ( eLBOW ): a tool for ligand coordinate and restraint generation journal September 2009
MolProbity : all-atom structure validation for macromolecular crystallography journal December 2009
Collaboration gets the most out of software journal September 2013
Dysregulation of Dual-Specificity Phosphatases by Epstein-Barr Virus LMP1 and Its Impact on Lymphoblastoid Cell Line Survival journal January 2020
Phthalimide conjugation as a strategy for in vivo target protein degradation journal May 2015
Targeted degradation of the enhancer lysine acetyltransferases CBP and p300 journal April 2021
Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy journal March 2021
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide journal January 2020
Structural reorganization of SHP2 by oncogenic mutations and implications for oncoprotein resistance to allosteric inhibition journal October 2018
Degradation of target protein in living cells by small-molecule proteolysis inducer journal February 2004
Delineating the role of cooperativity in the design of potent PROTACs for BTK journal July 2018
Development of selective small molecule MDM2 degraders based on nutlin journal August 2019
Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression journal December 2018
Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein journal May 2020
Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders journal June 2021