Small molecule allosteric modulators of mutant EGFR for non-small cell lung cancer therapy: An insight into design strategies and structure activity relationships.

Abstract excerpt

Non-small cell lung cancer (NSCLC) is one of the deadliest malignancies, which is mostly caused by activating mutations in the epidermal growth factor receptor (EGFR). While EGFR tyrosine kinase inhibitors (TKIs) of the first, second, and third generations have improved patient outcomes, long-term efficacy is often compromised by acquired resistance caused by mutations like T790 M and C797S. The discovery and...

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• Allosteric Regulation
• Drug Design
• Drug Screening Assays, Antitumor
• Molecular Structure
• Protein Kinase Inhibitors