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 article

2 Citations (Scopus)

Abstract

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
Volume19
Issue number23
DOIs
StatePublished - Jan 1 2019

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ras Proteins
Cell Membrane
Drug Repositioning
Drug Design
Biological Products
Cell Differentiation
Neoplasms
Cell Survival
Growth
Therapeutics
Lead

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery

Cite this

Recent Advances in Developing K-Ras Plasma Membrane Localization Inhibitors. / Ye, Na; Xu, Qingfeng; Li, Wanwan; Wang, Pingyuan; Zhou, Jia.

In: Current topics in medicinal chemistry, Vol. 19, No. 23, 01.01.2019, p. 2114-2127.

Research output: Contribution to journalReview article

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