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PHARMACOLOGICALLY ACTIVE MODIFIED SB101 MOLECULES AND USES THEREOF

机译:药理活性修饰的SB101分子及其用途

摘要

Modified SB 101 molecules with improved pharmacokinetic characteristics are provided. The pegylated protein has longer half life time than recombinant SB101-Fc fusion protein expressed in mammalian cells. The pegylated SB101 shows more than 70 times longer in vivo plasma half time and the fusion protein shows roughly 10 times longer half life time than unmodified SB101. Pegylated protein and fusion protein have maintained their in vitro activity similar to unmodified SB101. The SB101 fusion protein -molecules inhibit angiogenesis, block endothelial cell response to VEGF and inhibit VEGF receptor 2 protein. The modified molecules with improved pharmacokinetic characters are candidates for treatment of angiogenesis related diseases such as cancer.
机译:提供了具有改善的药代动力学特性的改性的SB 101分子。与在哺乳动物细胞中表达的重组SB101-Fc融合蛋白相比,聚乙二醇化蛋白的半衰期更长。聚乙二醇化的SB101的体内血浆半衰期延长了70倍以上,融合蛋白的半衰期大约是未修饰的SB101的10倍。聚乙二醇化蛋白和融合蛋白保持了与未修饰的SB101相似的体外活性。 SB101融合蛋白分子可抑制血管生成,阻断内皮细胞对VEGF的反应并抑制VEGF受体2蛋白。具有改善的药代动力学特征的修饰分子是用于治疗与血管生成有关的疾病例如癌症的候选物。

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