Small-molecule modulation of Ras signaling

Nat Chem Biol. 2014 Aug;10(8):613-22. doi: 10.1038/nchembio.1560. Epub 2014 Jun 15.

Abstract

Despite intense efforts in pharmaceutical industry and academia, a therapeutic grip on oncogenic Ras proteins has remained elusive. Mutated Ras is associated with ~20-30% of all human cancers often not responsive to established therapies. In particular, K-Ras, the most frequently mutated Ras isoform, is considered one of the most important but 'undruggable' targets in cancer research. Recently, new cavities on Ras for small-molecule ligands were identified, and selective direct targeting of mutated K-Ras(G12C) has become possible for what is to our knowledge the first time. In addition, impairment of Ras spatial organization, in particular via targeting the prenyl-binding Ras chaperone PDEδ, has opened a fresh perspective in anticancer research. These recent advances fuel hopes for the development of new drugs targeting Ras.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amino Acid Sequence
  • Guanosine Diphosphate / metabolism
  • Guanosine Triphosphate / metabolism
  • Humans
  • Molecular Sequence Data
  • Molecular Targeted Therapy
  • Mutation
  • Protein Conformation
  • Protein Kinases / metabolism
  • Signal Transduction* / drug effects
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / pharmacology
  • ras Proteins / antagonists & inhibitors*
  • ras Proteins / chemistry*
  • ras Proteins / genetics
  • ras Proteins / metabolism*

Substances

  • Small Molecule Libraries
  • Guanosine Diphosphate
  • Guanosine Triphosphate
  • Protein Kinases
  • cAMP phosphodiesterase kinase
  • ras Proteins