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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:Raf激酶蛋白二聚化和激酶活性的基于肽的抑制剂
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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:本文描述了用于修饰Raf激酶蛋白二聚化的基于肽的组合物。这些组合物,治疗和使用方法涉及对Raf激酶蛋白的二聚体界面表现出结合亲和力的肽,修饰Raf激酶二聚化的方法和抑制肿瘤生长的方法。本公开的一个实施方案是通过修饰选自SEQ ID NO:1的有序序列产生的肽,所述有序序列对应于B-Raf激酶的氨基酸503-521。本文公开的肽包括对源自SEQ ID NO:1的氨基酸的有序序列的修饰,其可以改善或改变所述肽与二聚体界面的结合亲和力。
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