PMID- 20939811 OWN - NLM STAT- MEDLINE DCOM- 20110704 LR - 20211203 IS - 1875-533X (Electronic) IS - 0929-8673 (Linking) VI - 17 IP - 35 DP - 2010 TI - PI3K/Akt/mTOR pathway inhibitors in cancer: a perspective on clinical progress. PG - 4326-41 AB - 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. FAU - Wu, P AU - Wu P AD - ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China. FAU - Hu, Y-Z AU - Hu YZ LA - eng PT - Journal Article PT - Review PL - United Arab Emirates TA - Curr Med Chem JT - Current medicinal chemistry JID - 9440157 RN - 0 (Antineoplastic Agents) RN - 0 (Phosphoinositide-3 Kinase Inhibitors) RN - 0 (Protein Kinase Inhibitors) RN - EC 2.7.11.1 (Proto-Oncogene Proteins c-akt) RN - EC 2.7.11.1 (TOR Serine-Threonine Kinases) SB - IM MH - Animals MH - Antineoplastic Agents/chemistry/metabolism/*pharmacology MH - Humans MH - Molecular Structure MH - Neoplasms/*drug therapy/metabolism MH - Phosphatidylinositol 3-Kinases/metabolism MH - *Phosphoinositide-3 Kinase Inhibitors MH - Protein Kinase Inhibitors/chemistry/metabolism/*pharmacology MH - Proto-Oncogene Proteins c-akt/*antagonists & inhibitors/metabolism MH - Structure-Activity Relationship MH - TOR Serine-Threonine Kinases/*antagonists & inhibitors/metabolism EDAT- 2010/10/14 06:00 MHDA- 2011/07/05 06:00 CRDT- 2010/10/14 06:00 PHST- 2010/07/27 00:00 [received] PHST- 2010/10/08 00:00 [accepted] PHST- 2010/10/14 06:00 [entrez] PHST- 2010/10/14 06:00 [pubmed] PHST- 2011/07/05 06:00 [medline] AID - BSP/CMC/E-Pub/ 268 [pii] AID - 10.2174/092986710793361234 [doi] PST - ppublish SO - Curr Med Chem. 2010;17(35):4326-41. doi: 10.2174/092986710793361234.