CFTR
CFTR (Cystic fibrosis transmembrane conductance regulator) is a membrane protein and chloride channel in vertebrates that is encoded by the CFTR gene. The CFTR gene codes for an ABC transporter-class ion channel protein that conducts chloride and thiocyanate ions across epithelial cell membranes. Mutations of the CFTR gene affecting chloride ion channel function lead to dysregulation of epithelial fluid transport in the lung, pancreas and other organs, resulting in cystic fibrosis.
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PFK-015是PFKFB3抑制剂,对重组PFKFB3的IC50为110 nM,能抑制肿瘤细胞内PFKFB3活性,IC50为20 nM。
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KU-55933 (ATM Kinase Inhibitor)是一种特异性的ATM抑制剂,IC50/Ki为12.9 nM/2.2 nM,与DNA-PK, PI3K/PI4K, ATR和mTOR相比,作用于ATM具有高度选择性。
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KU-60019是KU-55933的改良类似物,对ATM的IC50为6.3 nM。
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VE-821是一种选择性的,ATP竞争性ATR抑制剂,Ki/IC50为13 nM/26 nM,抑制H2AX磷酸化,对PIKKs ATM, DNA-PK, mTOR和PI3Kγ具有最低限度的抑制活性。
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五味子乙素是从五味子中分离联苯环辛二烯衍生物,已被证明对啮齿类动物的肝脏和心脏的抗氧化作用。
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