Oreganic acid: A potent novel inhibitor of Ras farnesyl-protein transferase from an endophytic fungus

被引：25

作者：

Jayasuriya, H ^{[1
]}

Bills, GF ^{[1
]}

Cascales, C ^{[1
]}

Zink, DL ^{[1
]}

Goetz, MA ^{[1
]}

Jenkins, RG ^{[1
]}

Silverman, KC ^{[1
]}

Lingham, RB ^{[1
]}

Singh, SB ^{[1
]}

机构：

[1] MERCK SHARP & DOHME ESPANA SA,CTR INVEST BASICA,MADRID 28027,SPAIN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 17期

关键词：

D O I：

10.1016/0960-894X(96)00372-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibitors of farnesyl-protein transferase (FPTase) have the potential of being anticancer agents for tumors in which ras is found mutated and contributes to cell transformation. From the screening of the extracts tricarboxylated alkylsulfate, oreganic acid (1), as a potent (IC50 = 14 nM) and specific inhibitor of FPTase. Its desulfated analog (4) was less active (IC50 = 3.3 mu M). The trimethylester (2) and its desulfated analog (3) were inactive. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：2081 / 2084

页数：4

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