申请人:The Arizona Disease Control Research Commission
公开号:US20030219847A1
公开(公告)日:2003-11-27
Prenylating enzymes are involved in modifying oncoproteins, such as RAS, so that growth of neoplastic cells becomes uncontrolled. Inactivation of such enzymes can prevent uncontrolled growth. &agr;-Dicarbonyl compounds can be used to covalently modify and thereby inactivate prenylating enzymes such as protein farnesyltransferase and protein geranylgeranyltransferase. The compounds can be designed to enhance affinity and/or specificity for a particular protein substrate.
前酰化酶参与修饰 RAS 等肿瘤蛋白,从而使肿瘤细胞的生长失控。二羰基化合物可用于共价修饰,从而使蛋白质法尼基转移酶和蛋白质香叶基转移酶等前酰化酶失活。化合物的设计可以增强对特定蛋白质底物的亲和力和/或特异性。