Technical Articles

KRAS小分子抑制剂的药物发现策略——从共价锁定到蛋白降解
Drug Discovery Strategies for KRAS Small-Molecule Inhibitors—From Covalent Locking to Protein Degradation
发布时间 2026-06-10
The development history of KRAS inhibitors spans over thirty years, with the first two decades nearly stagnant and the last decade witnessing an explosion. The turning point lies in the new understanding of KRAS's dynamic conformations and advancements in chemical technologies—particularly the application of covalent chemistry, fragment-based drug design, and targeted protein degradation.
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  • Immunity/Inflamma
  • KRAS inhibitors
  • covalent inhibitors
  • non-covalent inhibitors
  • PROTAC
  • molecular glues
  • fragment screening
  • high-throughput screening
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