Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4308-12. doi: 10.1016/j.bmcl.2010.05.099. Epub 2010 Jun 1.

Abstract

Over the past few years a number of components of the PI3K/mTOR pathway have been the subject of intense drug discovery activities both in pharmaceutical companies and in academia. This review article summarizes progress made in the identification and development of allosteric and ATP-competitive kinase inhibitors of mTOR and their potential therapeutic use in oncology.

Publication types

  • Review

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Allosteric Regulation
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / therapeutic use
  • Humans
  • Neoplasms / drug therapy*
  • Phosphatidylinositol 3-Kinase / metabolism
  • Phosphoinositide-3 Kinase Inhibitors
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / therapeutic use
  • Pyrimidines / chemistry
  • Pyrimidines / therapeutic use
  • Signal Transduction
  • TOR Serine-Threonine Kinases / antagonists & inhibitors*
  • TOR Serine-Threonine Kinases / metabolism

Substances

  • Antineoplastic Agents
  • Phosphoinositide-3 Kinase Inhibitors
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Adenosine Triphosphate
  • Phosphatidylinositol 3-Kinase
  • TOR Serine-Threonine Kinases