Authors: Wu, P.; Hu, Y.-Z.

Source: Current Medicinal Chemistry, Volume 17, Number 35, December 2010 , pp. 4326-4341(16)

Publisher: Bentham Science Publishers

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.

Keywords: PI3K; Akt/PKB; mTOR; small-molecule inhibitor; clinical; cancer; PKB; Akt; PDK-1; cancer therapy; FDA; kinases; cell growth; proliferation; apoptosis; transcription; translation; migration; motility; angiogenesis; immunity; metabolism; FRAP1; Raptor; Rictor; Erlotinib; Sunitinib; Nilotinib; eIF; S6Ks; Mcl-1; SGK1; PKC; Rapamycin; CCI-779; RCC; SCCHN; RAD-001; OSI-027; AZD-8055; PI3K INHIBITORS; GPCRs; Vps34; PIKKs; ATM; ATR; DNA-PK; SMG-1; TRRAP; GDC-0941

Document Type: Research article

DOI: http://dx.doi.org/10.2174/092986710793361234

Publication date: 2010-12-01

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• Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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