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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Tacrolimus (FK506)是一种免疫抑制剂和大环内酯类抗生素，用于同种异体的器官移植，可以降低病人的免疫系统的作用。
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Rapamycin, an mTOR inhibitor, shows potent immunosuppressive and antiproliferative properties. Rapamycin是一种常用的选择性的mTOR抑制剂，IC50为~0.1 nM。
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INK 128 (MLN0128)是一种有效的，选择性的mTOR抑制剂，IC50为1 nM；对I型PI3K亚型的作用效果低200倍以上，与Rapamycin相比，优先抑制mTORC1/2，且对促侵袭基因敏感。
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Palomid 529抑制mTORC1和mTORC2复合体，降低pAktS473， pGSK3βS9和pS6磷酸化，但是对pMAPK和pAktT308没有作用效果。
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WYE-125132是ATP竞争性mTOR选择性抑制剂，IC50为0.19 nM，对PI3Ks及其相关的hSMG1和ATR抑制性较弱。
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