PI3K/AKT/mTOR通路
mTORC2型
mTORC1型
蛋白激酶B
癌变
癌症研究
计算生物学
癌症
信号转导
化学
生物
细胞生物学
遗传学
作者
Rodrigo Dienstmann,Jordi Rodón,Ben Markman,Josep Tabernero
出处
期刊:Recent Patents on Anti-cancer Drug Discovery
[Bentham Science]
日期:2011-05-01
卷期号:6 (2): 210-236
被引量:23
标识
DOI:10.2174/157489211795328503
摘要
Inappropriate PI3K signaling is one of the most frequent occurrences in human cancer and is critical for tumor progression. A variety of genetic mutations and amplifications have been described affecting key components of this pathway, with implications not only for tumorigenesis but also for resistance to targeted agents. Emerging preclinical research has significantly advanced our understanding of the PI3K pathway and its complex downstream signalling, interactions and crosstalk. This knowledge, combined with the limited clinical antitumor activity of mTOR complex 1 inhibitors, has led to the development of rationally designed drugs targeting key elements of this pathway, such as pure PI3K inhibitors (both pan-PI3K and isoform-specific), dual PI3K/ mTOR inhibitors, Akt inhibitors, and mTOR complexes 1 and 2 catalytic site inhibitors. This review will focus primarily on an analysis of newly developed inhibitors of this pathway that have entered clinical trials, and recently registered patents in this field. Keywords: Cancer, drug development, mTORC1, mTORC2, PI3K, patent, protein kinase B/Akt
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