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    Method of inhibiting a farnesyl transferase enzyme
    10.
    发明授权
    Method of inhibiting a farnesyl transferase enzyme 失效
    抑制法呢基转移酶的方法

    公开(公告)号：US06790633B1

    公开(公告)日：2004-09-14

    申请号：US09665637

    申请日：2000-09-19

    申请人： Michael S. Brown ,  Joseph L. Goldstein ,  Yuval Reiss

    发明人： Michael S. Brown ,  Joseph L. Goldstein ,  Yuval Reiss

    IPC分类号： C12Q148

    CPC分类号： C07K1/1077 ,  A61K38/00 ,  C07K5/1013 ,  C07K5/1016 ,  C07K5/1019 ,  C07K5/1024 ,  C07K7/02 ,  C07K7/06 ,  C07K14/82 ,  C12N9/1085

    摘要： Disclosed are methods and compositions for the identification, characterization and inhibition of farnesyl protein transferases, enzymes involved in the farnesylation of various cellular proteins, including cancer related ras proteins such as p21ras. One farnesyl protein transferase which is disclosed herein exhibits a molecular weight of between about 70,000 and about 100,000 upon gel exclusion chromatography. The enzyme appears to comprise one or two subunits of approximately 50 kDa each. Methods are disclosed for assay and purification of the enzyme, as well as procedures for using the purified enzyme in screening protocols for the identification of possible anticancer agents which inhibit the enzyme and thereby prevent expression of proteins such as p21ras. Also disclosed is a families of compounds which act either as false substrates for the enzyme or as pure inhibitors and can therefore be employed for inhibition of the enzyme. The most potent inhibitors are ones in which phenylalanine occurs at the third position of a tetrapeptide whose amino terminus is cysteine.

    摘要翻译： 公开了用于鉴定，表征和抑制法呢基蛋白转移酶的方法和组合物，涉及各种细胞蛋白的法呢基化的酶，包括癌相关的ras蛋白如p21 。 本文公开的一种法呢基蛋白转移酶在凝胶排阻色谱上显示约70,000至约100,000的分子量。 该酶似乎包含一个或两个约50kDa的亚单位。 公开了用于酶的测定和纯化的方法，以及在筛选方案中使用纯化酶鉴定可能的抗癌剂的方法，所述抗癌剂抑制酶，从而阻止蛋白质如p21 的表达。 还公开了作为酶的假底物或纯抑制剂的化合物家族，因此可用于抑制酶。 最有效的抑制剂是其氨基末端是半胱氨酸的四肽的第三位发生苯丙氨酸的抑制剂。