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    • 7. 发明授权
    • Peptide antagonists of cellular mitogenesis and motogenesis and their therapeutic use
    • 细胞有丝分裂和机制的肽拮抗剂及其治疗用途
    • US06245742B1
    • 2001-06-12
    • US08930616
    • 1997-10-15
    • Carlo BattistiniPatrizia GiordanoSabrina De RosaFabio CorradiPaolo ComoglioAlberto Bardelli
    • Carlo BattistiniPatrizia GiordanoSabrina De RosaFabio CorradiPaolo ComoglioAlberto Bardelli
    • A61K3800
    • C07K5/0827C07K5/0202C07K5/1016C07K5/1027C07K14/71
    • The present invention relates to peptides and peptidomimetic compounds and pharmaceutical compositions containing them as useful pharmacological agents in the control or treatment of proliferative diseases such as cancer, against tumor growing and/or tumoral metastasis, and psoriasis and in the control or treatment of inflammatory, allergic, autoimmune, viral, and cardiovascular diseases. These new compounds have the unique property to inhibit the recognition of several phosphotyrosine containing motifs within all the cellular receptors and cytosolic transducers by a wide spectrum of SH2 domains contained in cytosolic transducers and other effector proteins laying along different pathways of the signal transduction process and with a particularly high affinity for the SH2 domain of the adaptor transducer Grb2, a key element along the pathway to mitogenesis and motogenesis, this last activity leading to invasiveness and to metastasis. The invention also relates to methods for production of the compounds and methods of treatment employing the compounds.
    • 本发明涉及肽和拟肽化合物和药物组合物,其含有它们作为控制或治疗增殖性疾病如癌症,抗肿瘤生长和/或肿瘤转移以及牛皮癣以及控制或治疗炎症, 过敏性,自身免疫性,病毒性和心血管疾病。 这些新化合物具有独特的性质,可以通过广泛的SH2结构域抑制所有细胞受体和细胞溶质转导体中识别的含有多种含磷酸酪氨酸基序,这些SH2结构域包含在信号转导过程不同途径的细胞溶质转导和其他效应蛋白中, 对于适应器传感器Grb2的SH2结构域特别高的亲和力,Grb2是沿着有丝分裂和发育的途径的关键因素,这是导致侵袭和转移的最后一个活动。 本发明还涉及化合物的制备方法和使用该化合物的处理方法。