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PBR ligand and its derivatives which can control the differentiation of adipocytic cells and composition for controling the differentiation of adipocytic cells comprising the same
PBR ligand and its derivatives which can control the differentiation of adipocytic cells and composition for controling the differentiation of adipocytic cells comprising the same
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机译:可以控制脂肪细胞分化的PBR配体及其衍生物和用于控制脂肪细胞分化的组合物
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摘要
PURPOSE: PBR ligand and its derivatives which control the differentiation of adipocytic cells and a composition for controlling the differentiation of adipocytic cells comprising the same are provided, which PBR(peripheral type benzodiazepine receptor) ligand inhibits growth of substrate cells and differentiation of the substrate cells into adipocytic cells, so that it can be useful for prevention and treatment of obeseness. CONSTITUTION: The PBR protein has the amino acid sequence of SEQ ID NO:1, is expressed from MSC(mesenchymal stem cell), and is associated with the control of the differentiation of adipocytic cells. A screening method of the PBR ligand comprises the steps of: treating the MSC expressing the PBR protein with a certain drug; and measuring the differentiation of the adipocytic cells in the MSC. The PBR ligand of formula (I) and its derivatives which control the differentiation of adipocytic cells are provided, wherein R1 is C1-C3 lower alkyl; R2 is aryl or halogenated aryl; and R3 is halogen atom. The composition for controlling the differentiation of adipocytic cells comprises 1 to 10 microM or 20 to 50 microM of the PBR ligand of formula (I) and its derivatives for inducing or inhibiting the differentiation of adipocytic cells.
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机译:用途:提供控制脂肪细胞分化的PBR配体及其衍生物,以及包含其的控制脂肪细胞分化的组合物,其中PBR(外周型苯并二氮杂receptor受体)配体抑制基质细胞的生长和基质细胞的分化。进入脂肪细胞,因此可用于预防和治疗肥胖症。组成:PBR蛋白具有SEQ ID NO:1的氨基酸序列,由间充质干细胞(MSC)表达,并与脂肪细胞的分化控制有关。 PBR配体的筛选方法包括以下步骤:用某种药物处理表达PBR蛋白的MSC。并测量MSC中脂肪细胞的分化。提供了控制脂肪细胞分化的式(I)的PBR配体及其衍生物,其中R1为C1-C3低级烷基; R2是芳基或卤代芳基; R 3为卤素原子。用于控制脂肪细胞分化的组合物包含1至10μM或20至50μM的式(I)的PBR配体及其衍生物,用于诱导或抑制脂肪细胞的分化。
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