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

Design of a ?Two-in-One? Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the

Journal Article · · J. Med. Chem.
; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ; ;

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:
1854251
Journal Information:
J. Med. Chem., Vol. 65, Issue (2)
Country of Publication:
United States
Language:
ENGLISH

References (32)

A decade of EGFR inhibition in EGFR-mutated non small cell lung cancer (NSCLC): Old successes and future perspectives journal June 2015
Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to Gefitinib journal May 2004
EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy journal June 2004
Activating and resistance mutations of EGFR in non-small-cell lung cancer: role in clinical response to EGFR tyrosine kinase inhibitors journal August 2009
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP journal January 2008
EGFR Mutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib journal February 2005
Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain journal February 2005
Analysis of Tumor Specimens at the Time of Acquired Resistance to EGFR-TKI Therapy in 155 Patients with EGFR -Mutant Lung Cancers journal March 2013
Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib journal May 2005
AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer journal June 2014
Osimertinib in Untreated EGFR -Mutated Advanced Non–Small-Cell Lung Cancer journal January 2018
Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M journal May 2015
Lung Cancer: EGFR Inhibitors with Low Nanomolar Activity against a Therapy-Resistant L858R/T790M/C797S Mutant journal July 2016
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site journal June 2017
Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping journal May 2017
Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors journal April 2020
Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer: Miniperspective journal November 2017
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
Full Functionalization of the Imidazole Scaffold by Selective Metalation and Sulfoxide/Magnesium Exchange journal December 2013
Extending Pummerer Reaction Chemistry: Studies in the Palau’amine Synthesis Area journal May 2011
Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR L858R/T790M/C797S journal May 2019
Targeting Her2-insYVMA with Covalent Inhibitors—A Focused Compound Screening and Structure-Based Design Approach journal September 2020
Design, Synthesis, and Pharmacological Evaluation of Novel Hybrid Compounds To Treat Sickle Cell Disease Symptoms journal July 2011
Structures of Lung Cancer-Derived EGFR Mutants and Inhibitor Complexes: Mechanism of Activation and Insights into Differential Inhibitor Sensitivity journal March 2007
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M journal December 2009
Target engagement and drug residence time can be observed in living cells with BRET journal December 2015
Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement journal February 2018
Glide:  A New Approach for Rapid, Accurate Docking and Scoring. 1. Method and Assessment of Docking Accuracy journal March 2004
Glide:  A New Approach for Rapid, Accurate Docking and Scoring. 2. Enrichment Factors in Database Screening journal March 2004
Extra Precision Glide:  Docking and Scoring Incorporating a Model of Hydrophobic Enclosure for Protein−Ligand Complexes journal October 2006

Similar Records

Related Subjects