ArticleAngewandte Chemie (International ed. in English)2018
Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.
Article in Angewandte Chemie (International ed. in English), 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 1 synthesis or guideline pooled it, 29 citations in OpenAlex.
- Therapeutic exploration of uncommon EGFR exon 20 insertion mutations in advanced non-small cell lung cancer: breaking through brambles and thorns.Journal of cancer research and clinical oncology · 2022Pooled it
- Analysis of the efficacy and influencing factors of double-dose furmonertinib for advanced EGFR ex20ins non-small cell lung cancer.Journal of translational medicine · 2025Article
- Discovery of STX-721, a Covalent, Potent, and Highly Mutant-Selective EGFR/HER2 Exon20 Insertion Inhibitor for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry · 2025Article
- The current landscape, advancements, and prospects in the treatment of patients with EGFR exon 20 insertion mutations warrant scientific elucidation.Frontiers in oncology · 2024Review
- Non-small Cell Lung Cancer with EGFR or HER2 Exon 20 Insertion Mutations: Diagnosis and Treatment Options.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy · 2022Review
- Allele-specific activation, enzyme kinetics, and inhibitor sensitivities of EGFR exon 19 deletion mutations in lung cancer.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- EGFR and HER2 exon 20 insertions in solid tumours: from biology to treatment.Nature reviews. Clinical oncology · 2022Review
- Identification of Potential Core Genes Between Primary and Metastatic Malignant Melanoma and Analysis of Their Immune Correlation.International journal of general medicine · 2022Article
- Treatment of Brain Metastases of Non-Small Cell Lung Carcinoma.International journal of molecular sciences · 2021Review
- Clinical Characteristics and Prognosis of HER2 Gene Phenotype in Patients with Non-Small Cell Lung Cancer.International journal of general medicine · 2021Article
- Identification of novel bioactive molecules from garlic bulbs: A special effort to determine the anticancer potential against lung cancer with targeted drugs.Saudi journal of biological sciences · 2020Article
- Combination effects of ellagic acid with erlotinib in a Ba/F3 cell line expressing EGFR H773_V774 insH mutation.Thoracic cancer · 2020Article
- Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.Journal of medicinal chemistry · 2020Article
- Rare epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer.Seminars in cancer biology · 2020Review
- How Different Substitution Positions of F, Cl Atoms in Benzene Ring of 5-Methylpyrimidine Pyridine Derivatives Affect the Inhibition Ability of EGFRMolecules (Basel, Switzerland) · 2020Article
- TargetingSignal transduction and targeted therapyReview
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
Abstract
Exon 20 insertion (Ex20Ins) mutations are the third most prevalent epidermal growth factor receptor (EGFR) activating mutation and the most prevalent HER2 mutation in non-small cell lung cancer (NSCLC). Novel therapeutics for the patients with Ex20Ins mutations are urgently needed, due to their poor responses to the currently approved EGFR and HER2 inhibitors. Here we report the discovery of highly potent and broadly effective EGFR and HER2 Ex20Ins mutant inhibitors. The co-crystal structure of compound 1 b in complex with wild type EGFR clearly revealed an additional hydrophobic interaction of 4-fluorobenzene ring within a deep hydrophobic pocket, which has not been widely exploited in the development of EGFR and HER2 inhibitors. As compared with afatinib, compound 1 a exhibited superior inhibition of proliferation and signaling pathways in Ba/F3 cells harboring either EGFR or HER2 Ex20Ins mutations, and in the EGFR P772_H773insPNP patient-derived lung cancer cell line DFCI127. Our study identifies promising strategies for development of EGFR and HER2 Ex20Ins mutant inhibitors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.