Recent advances in developing K-ras plasma membrane localization inhibitors

Na Ye, Qingfeng Xu, Wanwan Li, Pingyuan Wang, Jia Zhou

Research output: Contribution to journalReview articlepeer-review

4 Scopus citations


The Ras proteins play an important role in cell growth, differentiation, proliferation and survival by regulating diverse signaling pathways. Oncogenic mutant K-Ras is the most frequently mutated class of Ras superfamily that is highly prevalent in many human cancers. Despite intensive efforts to combat various K-Ras-mutant-driven cancers, no effective K-Ras-specific inhibitors have yet been approved for clinical use to date. Since K-Ras proteins must be associated to the plasma membrane for their function, targeting K-Ras plasma membrane localization represents a logical and potentially tractable therapeutic approach. Here, we summarize the recent advances in the development of K-Ras plasma membrane localization inhibitors including natural product-based inhibitors achieved from high throughput screening, fragment-based drug design, virtual screening, and drug repurposing as well as hit-to-lead optimizations.

Original languageEnglish (US)
Pages (from-to)2114-2127
Number of pages14
JournalCurrent topics in medicinal chemistry
Issue number23
StatePublished - 2019


  • Cancer
  • Drug discovery
  • K-Ras
  • K-Ras mutation
  • Plasma membrane localization inhibitors
  • RAS

ASJC Scopus subject areas

  • Drug Discovery


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