mTOR
mTOR (mechanistic target of rapamycin) is a member of the phosphatidylinositol 3-kinase-related kinase family of protein kinases.mTOR functions as a serine/threonine protein kinase that regulates cell growth, cell proliferation, cell motility, cell survival, protein synthesis, autophagy, and transcription.mTOR integrates the input from upstream pathways, including insulin, growth factors (such as IGF-1 and IGF-2), and amino acids. mTOR also senses cellular nutrient, oxygen, and energy levels. The mTOR pathway is a central regulator of mammalian metabolism and physiology, with important roles in the function of tissues including liver, muscle, white and brown adipose tissue, and the brain, and is dysregulated in human diseases, such as diabetes, obesity, depression, and certain cancers. MTOR is the catalytic subunit of two structurally distinct complexes: mTORC1 and mTORC2. Both complexes localize to different subcellular compartments, thus affecting their activation and function. As a core component of mTORC2, mTOR also functions as a tyrosine protein kinase that promotes the activation of insulin receptors and insulin-like growth factor 1 receptors. mTORC2 has also been implicated in the control and maintenance of the actin cytoskeleton.
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OSI-027是mTORC1和mTORC2选择性抑制剂，IC50为22 nM和65 nM，比对PI3Kα，PI3Kβ，PI3Kγ和DNA-PK的抑制性高100倍。
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WYE-354是ATP竞争性mTOR抑制剂，IC50为5 nM，能阻断mTORC1/P-S6K(T389)和mTORC2/P-AKT(S473)，比对PI3Kα和PI3Kγ的抑制性强100倍和500倍。
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Torin 1是一种有效的mTORC1/2抑制剂，IC50为2 nM/10 nM；作用于mTOR比作用于PI3K选择性高1000倍。
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Temsirolimus (CCI-779) is a specific mTOR inhibitor with IC50 of 1.76 μM。
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AZD8055是一种新型的，ATP竞争性的mTOR抑制剂，IC50为0.8 nM，与作用于PI3K亚型和ATM/DNA-PK相比，具有优异的选择性（约1000倍）。
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