ISOLATION AND STRUCTURE OF CHAETOMELLIC ACIDS A AND B FROM CHAETOMELLA-ACUTISETA - FARNESYL PYROPHOSPHATE MIMIC INHIBITORS OF RAS FARNESYL-PROTEIN TRANSFERASE

被引:112
作者
SINGH, SB
ZINK, DL
LIESCH, JM
GOETZ, MA
JENKINS, RG
NALLINOMSTEAD, M
SILVERMAN, KC
BILLS, GF
MOSLEY, RT
GIBBS, JB
ALBERSSCHONBERG, G
LINGHAM, RB
机构
[1] Merck Research Laboratories, Rahway, NJ 07065
关键词
CHAETOMELLIC ACIDS; RAS FPTASE INHIBITORS; FPP MIMIC; CHAETOMELLA-ACUTISETA;
D O I
10.1016/S0040-4020(01)87178-7
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Farnesyl-Protein transferase catalyses a post-translational modification of Ras that is obligatory for the cell transforming activity of this oncogene protein. The screening of natural products to identify inhibitors of this enzyme as a potential anticancer agents, has led to the isolation of two novel dicarboxylic acids, named chaetomellic acids from Chaetomella acutiseta , as potent and selective inhibitors which appear to be the first examples of non-phosphorous containing FPP mimics.
引用
收藏
页码:5917 / 5926
页数:10
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