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    • 8. 发明申请
    • GROWTH FACTOR RECEPTOR-LIKE PEPTIDES WITHOUT TYROSINE-KINASE ACTIVITY
    • 不含酪氨酸激酶活性的生长因子受体样肽
    • WO1990008160A1
    • 1990-07-26
    • PCT/GB1990000083
    • 1990-01-19
    • IMPERIAL CANCER RESEARCH TECHNOLOGY LTD.STERNBERG, Michael, Joseph, EzraGULLICK, William, JohnCHOTHIA, Cyrus
    • IMPERIAL CANCER RESEARCH TECHNOLOGY LTD.
    • C07K07/08
    • C07K14/82A61K38/00C07K14/71
    • A peptide which lacks tyurosine kinase activity, having a binding portion of at least 8 contiguous amino acid residues adapted to form an intra-membrane alpha-helix and being capable of reducing tyrosine kinase activity in a target cell, the binding portion having a sequence identical to the sequence at positions P to P of a natural (wild type) or mutant growth factor receptor/tyrosine kinase portein having the motif set out below or having a sequence which differs at not more than 3 positions from the sequence at positions P to P of such a protein, wherein the motif comprises a sequence of 5 contiguous amino acid residues designated: P XXP P , wherein the residues X are the same or different and each is any naturally occurring L-amino acid residue, P is a residue selected from Ala, Gly, Ser, Thr, Pro, Val, Ile and leu, P is a residue selected from Ala, Gly, Met, Val, Ile and Leu and P is a residue selected from Ala, Gly, Thr, Pro and Val.
    • 缺乏酪氨酸激酶活性的肽,其具有适于形成膜内α-螺旋的至少8个连续氨基酸残基的结合部分,并且能够降低靶细胞中的酪氨酸激酶活性,所述结合部分具有相同的序列 至具有以下所示基序的天然(野生型)或突变型生长因子受体/酪氨酸激酶蛋白的位置P 0至P 7的序列,或具有不超过3个位置的序列 该蛋白质的位置P <0>至P <7>的序列,其中所述基序包含指定为:P P P P 4的5个连续氨基酸残基的序列,其中残基X为 相同或不同,并且各自是任何天然存在的L-氨基酸残基,P 0是选自Ala,Gly,Ser,Thr,Pro,Val,Ile和leu的残基,P 3是选自Ala ,Gly,Met,Val,Ile和Leu,P 4是选自Ala,Gly,Thr,Pro和Val的残基。