Structural pharmacological studies on EGFR T790M/C797S.
Sign Up to like & getrecommendations! Published in 2017 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2017.04.138
Abstract: Drug-resistance is a major challenge in targeted therapy of EGFR mutated non-small cell lung cancers (NSCLCs). The third-generation irreversible inhibitors such as AZD9291, CO-1686 and WZ4002 can overcome EGFR T790M drug-resistance mutant through covalent binding… read more here.
Keywords: structural pharmacological; egfr t790m; pharmacological studies; t790m c797s ... See more keywords
Crystal structure of EGFR T790M/C797S/V948R in complex with EAI045.
Sign Up to like & getrecommendations! Published in 2018 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2018.05.154
Abstract: Lung cancer is the leading cause of cancer deaths. Epidermal growth factor receptor (EGFR) kinase domain mutations are a common cause of non-small cell lung cancers (NSCLCs), a major subtype of lung cancers. Patients harboring… read more here.
Keywords: structure; egfr t790m; v948r complex; t790m c797s ... See more keywords
Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00168
Abstract: Tertiary C797S mutation of epidermal growth factor receptor (EGFR)-mediated resistance in non-small-cell-lung-cancer (NSCLC) patients is still an unmet clinical need. Several classes of adenosine 5'-triphosphate-competitive or allosteric EGFRT790M/C797S inhibitors and degraders have been developed, but… read more here.
Keywords: c797s; factor receptor; epidermal growth; growth factor ... See more keywords
Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting Del19/T790M/C797S Mutation.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.1c00645
Abstract: The tertiary epidermal growth factor receptor (EGFR) C797S mutation predominates in the acquired mutational resistance in cancer patients to third-generation EGFR inhibitors. Small-molecule inhibitors targeting the EGFR C797S mutation have been developed with good efficiency.… read more here.
Keywords: t790m c797s; egfr; c797s; c797s mutation ... See more keywords
Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S††Electronic supplementary information (ESI) available. CCDC 1876852. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c9sc03445e
Sign Up to like & getrecommendations! Published in 2019 at "Chemical Science"
DOI: 10.1039/c9sc03445e
Abstract: We present inhibitors of drug resistant mutants of EGFR including T790M and C797S. In addition, we present the first X-ray crystal structures of covalent inhibitors in complex with C797S-mutated EGFR to gain insight into their… read more here.
Keywords: osimertinib resistant; c797s; t790m c797s; esi ... See more keywords
Abstract 4018: BBT-207 is a broad-spectrum, highly potent, 4th generation EGFR TKI with enhanced activity to both sensitizing and treatment-emergent EGFR mutations including T790M and C797S
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-4018
Abstract: Background: EGFR mutation in non-small cell lung cancer (NSCLC) presents a viable therapeutic target for which tyrosine kinase inhibitor (TKI) therapy has shown impressive clinical benefit over the past 20 years. Unfortunately, most patients inevitably… read more here.
Keywords: bbt 207; t790m c797s; generation; activity ... See more keywords
The concomitant EGFR T790M/C797S in trans and cis in three osimertinib-resistant lung adenocarcinoma patients.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2019.37.15_suppl.e20105
Abstract: e20105 Background: EGFR C797S mutation is an important cause of Osimertinib resistance. Previous studies showed that patients harboring EGFR C797S in trans with T790M are sensitive to a combination of first- and third-generation EGFR tyrosine… read more here.
Keywords: egfr t790m; c797s; c797s trans; trans cis ... See more keywords
Quinoxalinones as A Novel Inhibitor Scaffold for EGFR (L858R/T790M/C797S) Tyrosine Kinase: Molecular Docking, Biological Evaluations, and Computational Insights
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules27248901
Abstract: Combating acquired drug resistance of EGFR tyrosine kinase (TK) is a great challenge and an urgent necessity in the management of non-small cell lung cancers. The advanced EGFR (L858R/T790M/C797S) triple mutation has been recently reported,… read more here.
Keywords: t790m c797s; l858r t790m; egfr l858r;