Abstract
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 language | English |
|---|---|
| Journal | Current Medicinal Chemistry |
| Volume | 17 |
| Issue number | 35 |
| Pages (from-to) | 4326-4341 |
| ISSN | 0929-8673 |
| DOIs | |
| Publication status | Published - 2010 |
| Externally published | Yes |
Keywords
- 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
