Discovery of Potent EGFR Inhibitors for Del19 and L858R/T790M Mutants Through Structure-Based Virtual Screening and Biological Evaluation.

doi:10.1111/cbdd.70391

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Discovery of Potent EGFR Inhibitors for Del19 and L858R/T790M Mutants Through Structure-Based Virtual Screening and Biological Evaluation.

Chemical biology & drug design - 1 Sept 2026

Xu Ting, Zhao Yuchen, Chen Mengfei, Zuo Lijuan, Cai Hanshuang, Liu Yuguo, Liu Chuanfeng, Shi Jing

Abstract excerpt

Epidermal growth factor receptor (EGFR) mutation-mediated drug resistance represents a major clinical challenge in the treatment of non-small cell lung cancer (NSCLC). In this study, the lead compound XJ2-2 was identified through structure-based virtual screening. It exhibited potent anti-proliferative activity against both EGFRDel19 mutant PC-9 cells and EGFRL858R/T790M mutant H1975 cells, with IC50 values of...

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Topics

ErbB Receptors
Humans
Animals
Protein Kinase Inhibitors
Cell Line, Tumor
Lung Neoplasms

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

Mutation

Mice

Antineoplastic Agents

Carcinoma, Non-Small-Cell Lung

Molecular Docking Simulation

Cell Proliferation

Drug Resistance, Neoplasm

Structure-Activity Relationship

Source

Open in PubMed Open full text

Identifiers

PMID: 42723470
DOI: 10.1111/cbdd.70391
PMCID: PMC13563102

Genes

EGFR
PC

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 25 Oct 2026.

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