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Peptide based inhibitors of Raf kinase protein dimerization and kinase activity
Peptide based inhibitors of Raf kinase protein dimerization and kinase activity
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机译:基于肽的RAF激酶蛋白二聚化和激酶活性的抑制剂
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摘要
Herein are described peptide-based compositions for modifying Raf kinase protein Dimerization. These compositions, treatments, and methods of use are directed to peptides that display a binding affinity for the dimer interface of a Raf kinase protein, methods for modifying Raf kinase dimerization, and methods for inhibiting tumor growth. An embodiment of the disclosure is a peptide generated by modifying an ordered sequence chosen from SEQ ID NO: 1 which corresponds to amino acids 503-521 of B-Raf kinase. The peptides disclosed herein include a modification to an ordered sequence of amino acids derived from SEQ ID NO: 1 that can improve or otherwise alter binding affinity of the peptide to the dimer interface.
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机译:本文描述了基于肽的组合物,用于改变RAF激酶蛋白质二聚化。 使用这些组合物,处理和使用方法涉及显示RAF激酶蛋白的二聚体界面,改变RAF激酶二聚化的方法的结合亲和力的肽,以及用于抑制肿瘤生长的方法。 本公开的一个实施方案是通过修饰从SEQ ID NO:1中选择的有序序列产生的肽,其对应于B-RAF激酶的氨基酸503-521。 本文公开的肽包括对衍生自SEQ ID NO:1的有序氨基酸序列的修饰,其可以改善或以其他方式改变肽与二聚体界面的结合亲和力。
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