PI3K/Akt/mTOR Pathway Inhibitors in Cancer: A Perspective on Clinical Progress

Peng Wu, Y-Z Hu

Research output: Contribution to journalJournal articleResearchpeer-review


The phosphoinositide 3-kinase (PI3K)/serine-theronine protein kinase Akt (also known as protein kinase B (PKB))/mammalian target of rapamycin (mTOR) pathway is a vital transduction cascade that is connected with many essential cellular activities, such as growth and survival. Along with extensive pharmacological studies validating the therapeutic potential of targeting the PI3K/Akt/mTOR pathway for the treatment of cancer, kinase inhibitors targeting significant knots of this pathway including PI3K, Akt, mTOR, and 3-phosphoinositide-dependent protein kinase-1 (PDK-1) keep arising and entering clinical studies. Herein, we review the most up-to-date landscape on developing small-molecule kinase inhibitors targeting the PI3K/Akt/mTOR pathway, with emphasis on small-molecule inhibitors which have been progressed into clinical studies.
Original languageEnglish
JournalCurrent Medicinal Chemistry
Issue number35
Pages (from-to)4326-4341
Publication statusPublished - 2010
Externally publishedYes


  • biochemical pathway
  • transduction cascade
  • cancer Neoplasms (MeSH) neoplastic disease etiology, mortality
  • Primates Mammalia Vertebrata Chordata Animalia (Animals, Chordates, Humans, Mammals, Primates, Vertebrates) - Hominidae [86215] human common aged/80 and over
  • 3-phosphoinositide-dependent protein kinase-1 191808-15-8
  • mammalian target of rapamycin mTOR 171715-28-9
  • phosphoinositide 3-kinase/serine-theronine protein kinase PI3K/Akt
  • small-molecule kinase inhibitor
  • 10060, Biochemistry studies - General
  • 24004, Neoplasms - Pathology, clinical aspects and systemic effects
  • 24500, Gerontology
  • Human Medicine, Medical Sciences
  • Biochemistry and Molecular Biophysics
  • Oncology


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