ArticleJournal of chemical information and modeling2019
Structural Insights into Characterizing Binding Sites in Epidermal Growth Factor Receptor Kinase Mutants.
Article in Journal of chemical information and modeling, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 23 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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
23 citing papers in PubMed, 52 citations in OpenAlex.
- From virtual screening to cell-based assays: structure-guided identification of EGFR-targeting perimidine derivatives with anticancer activity.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- EGFR Mutations and Tyrosine Kinase Inhibitors: Structural Insights and Therapeutic Advances.ACS omega · 2026Review
- A Review on EGFR-Tyrosine Kinase Inhibitors and their Resistance Mechanisms.Current pharmaceutical design · 2026Review
- Thiourea Derivatives for the Potential Treatment of Lung Cancer via the Inhibition of EGFR and Efflux Pumps: Synthesis,Anti-cancer agents in medicinal chemistry · 2026Article
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- In silico exploration of anticancer plant phytochemicals for EGFR-targeted lung cancer therapy.Scientific reports · 2025Article
- Design and investigation of novel iridoid-based peptide conjugates for targeting EGFR and its mutants L858R and T790M/L858R/C797S: an in silico study.Molecular diversity · 2025Article
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- Evaluation of Cytotoxicity and Metabolic Profiling ofBiology · 2024Article
- Imidazole[1,5-a]pyridine derivatives as EGFR tyrosine kinase inhibitors unraveled by umbrella sampling and steered molecular dynamics simulations.Scientific reports · 2024Article
- Niosomes as promising approach for enhancing the cytotoxicity of Hemimycale sp. total crude extract supported with in-silico studies.Scientific reports · 2024Article
- Design, synthesis, docking, MD simulations, and anti-proliferative evaluation of thieno[2,3-Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Paralemnalia thyrsoides-associated fungi: phylogenetic diversity, cytotoxic potential, metabolomic profiling and docking analysis.BMC microbiology · 2023Article
- A Closer Look at EGFR Inhibitor Resistance in Non-Small Cell Lung Cancer through the Lens of Precision Medicine.Journal of clinical medicine · 2023Review
- Article
- Structural Insight and Development of EGFR Tyrosine Kinase Inhibitors.Molecules (Basel, Switzerland) · 2022Review
- Unlocking phenotypic plasticity provides novel insights for immunity and personalized therapy in lung adenocarcinoma.Frontiers in genetics · 2022Article
- In silico studies of interactions of peptide-conjugated cholesterol metabolites and betulinic acid with EGFR, LDR, and N-terminal fragment of CCKA receptors.Journal of molecular modeling · 2021Article
Corrections and comments
- Erratum issued
Authors and funding
3 authors at 2 institutions in 1 country.
Funding
Abstract
Over the last two decades epidermal growth factor receptor (EGFR) kinase has become an important target to treat nonsmall cell lung cancer (NSCLC). Currently, three generations of EGFR kinase-targeted small molecule drugs have been FDA approved. They nominally produce a response at the start of treatment and lead to a substantial survival benefit for patients. However, long-term treatment results in acquired drug resistance and further vulnerability to NSCLC. Therefore, novel EGFR kinase inhibitors that specially overcome acquired mutations are urgently needed. To this end, we carried out a comprehensive study of different EGFR kinase mutants using a structural systems pharmacology strategy. Our analysis shows that both wild-type and mutated structures exhibit multiple conformational states that have not been observed in solved crystal structures. We show that this conformational flexibility accommodates diverse types of ligands with multiple types of binding modes. These results provide insights for designing a new generation of EGFR kinase inhibitor that combats acquired drug-resistant mutations through a multiconformation-based drug design strategy.
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What OpenQuestion holds
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.