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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Torin 2是高活性mTOR选择性抑制剂，IC50为0.25 nM，比对PI3K的抑制性强800倍，有较好的药代动力学特性，还能抑制ATM，ATR和DNA-PK，EC50分别为28 nM，35 nM和118 nM。
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Everolimus (RAD001)是一种mTOR抑制剂，作用于FKBP12，IC50为1.6-2.4 nM。
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MHY1485是mTOR活化剂，能抑制自噬。
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PP242是mTOR选择性抑制剂，IC50为8 nM，比对PI3Kδ和PI3Kα/β/γ的抑制性高10倍和100倍，对BRD4有较弱抑制性，Kd为1.7 uM。
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KU-0063794是一种有效的，高度特异性的，作用于mTORC1和mTORC2的双重mTOR抑制剂，IC50约为~10 nM；对PI3Ks没有作用。
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