skip to main content
OSTI.GOV title logo U.S. Department of Energy
Office of Scientific and Technical Information

Title: Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors

Journal Article · · Nat. Commun.

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)
OSTI ID:
1872629
Journal Information:
Nat. Commun., Vol. 13
Country of Publication:
United States
Language:
ENGLISH

References (46)

Determining EGFR-TKI sensitivity of G719X and other uncommon EGFR mutations in non-small cell lung cancer: Perplexity and solution journal January 2017
Mechanistic insights into the activation of oncogenic forms of EGF receptor journal November 2011
Oncogenic Mutations Counteract Intrinsic Disorder in the EGFR Kinase and Promote Receptor Dimerization journal May 2012
EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy journal June 2004
Structural and mechanistic underpinnings of the differential drug sensitivity of EGFR mutations in non-small cell lung cancer journal March 2010
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP journal January 2008
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models journal April 2008
Phase I Trial of the Irreversible EGFR and HER2 Kinase Inhibitor BIBW 2992 in Patients With Advanced Solid Tumors journal September 2010
Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor journal October 2014
AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer journal June 2014
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M journal December 2009
Drug combination approach to overcome resistance to EGFR tyrosine kinase inhibitors in lung cancer journal October 2017
Osimertinib in Untreated EGFR -Mutated Advanced Non–Small-Cell Lung Cancer journal January 2018
Lessons To Be Learned: The Molecular Basis of Kinase-Targeted Therapies and Drug Resistance in Non-Small Cell Lung Cancer journal January 2018
The next tier of EGFR resistance mutations in lung cancer journal October 2020
Genomic landscape of acquired resistance to third‐generation EGFR tyrosine kinase inhibitors in EGFR T790M‐mutant non–small cell lung cancer journal March 2020
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors journal May 2016
Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors journal October 2019
Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor journal May 2019
An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer journal April 2022
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1 journal August 2018
Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors journal January 2010
Combining the Allosteric Inhibitor Asciminib with Ponatinib Suppresses Emergence of and Restores Efficacy against Highly Resistant BCR-ABL1 Mutants journal October 2019
Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands journal November 2020
On-target Resistance to the Mutant-Selective EGFR Inhibitor Osimertinib Can Develop in an Allele-Specific Manner Dependent on the Original EGFR-Activating Mutation journal February 2019
Conformational Preferences of π–π Stacking Between Ligand and Protein, Analysis Derived from Crystal Structure Data Geometric Preference of π–π Interaction journal September 2015
Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed journal December 2015
Exact Analysis of Heterotropic Interactions in Proteins: Characterization of Cooperative Ligand Binding by Isothermal Titration Calorimetry journal September 2006
Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors journal November 2019
Polytherapy and Targeted Cancer Drug Resistance journal March 2019
Combination therapy in combating cancer journal March 2017
Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer journal October 2006
The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1 journal March 2017
Structural Basis for the Autoinhibition of c-Abl Tyrosine Kinase journal March 2003
A Myristoyl/Phosphotyrosine Switch Regulates c-Abl journal March 2003
Cooperativity Between Orthosteric Inhibitors and Allosteric Inhibitor 8-Anilino-1-Naphthalene Sulfonic Acid (ANS) in Cyclin-Dependent Kinase 2 journal May 2020
Mechanisms of cutaneous toxicities to EGFR inhibitors journal October 2006
Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies journal March 2020
xia2 : an expert system for macromolecular crystallography data reduction journal December 2009
DIALS : implementation and evaluation of a new integration package journal February 2018
XDS journal January 2010
Overview of the CCP 4 suite and current developments journal March 2011
Features and development of Coot journal March 2010
PHENIX: a comprehensive Python-based system for macromolecular structure solution journal January 2010
electronic Ligand Builder and Optimization Workbench ( eLBOW ): a tool for ligand coordinate and restraint generation journal September 2009
Gefitinib Induces Apoptosis in the EGFR L858R Non–Small-Cell Lung Cancer Cell Line H3255 journal October 2004