Ras farnesyltransferase inhibition: a novel and safe approach for cancer chemotherapy  

抑制ras法尼基转移酶:一种新的、安全的肿瘤化疗方法(英文)

作　　者：Srinivas NAMMI Durga Srinivas LODAGALA 

机构地区：[1]Pharmacology Division,Department of Pharmaceutical Sciences,Andhra University,Visakhapatnam 530003 Andhra Pradesh,India,Pharmacology Division,Department of Pharmaceutical Sciences,Andhra University,Visakhapatnam 530003 Andhra Pradesh,India

出　　处：《Acta Pharmacologica Sinica》2000年第5期14-22,共9页中国药理学报（英文版）

摘　　要：The 21-kDa Ras proteins are well known for their regulatory role in oncogenic, mitogenic, and developmental signaling pathways. GTP activated Ras interacts directly with the Raf protein to recruit the MAP kinases and their subordinates. Attachment of Ras protein to the plasma membrane that requires farnesylation by farnesyl pyrophosphate at its C-terminus, is essential for its biological activity. Ras oncogenes are associated with a wide variety of solid tumors and leukemias for which existing chemotherapeutics have limited utility. A . promising pharmacological approach of antagonizing oncogenic Ras activity is to develop inhibitors of farnesyl transferase. These inhibitors may be useful in blocking the action of Ras onco-proteins.The 21-kDa Ras proteins are well known for their regulatory role in oncogenic, mitogenic, and developmental signaling pathways. GTP activated Ras interacts directly with the Raf protein to recruit the MAP kinases and their subordinates. Attachment of Ras protein to the plasma membrane that requires farnesylation by farnesyl pyrophosphate at its C-terminus, is essential for its biological activity. Ras oncogenes are associated with a wide variety of solid tumors and leukemias for which existing chemotherapeutics have limited utility. A . promising pharmacological approach of antagonizing oncogenic Ras activity is to develop inhibitors of farnesyl transferase. These inhibitors may be useful in blocking the action of Ras onco-proteins.

关 键 词：proto-oncogene protein p21 ( ras ) dimethylallyltranstransferase protein isoprenylation Ca2 +-calmodulin dependent protein kinase antineoplastic agents signal transduction 

分 类 号：R730.5[医药卫生—肿瘤]