FUSIDIENOL - A NOVEL INHIBITOR OF RAS FARNESYL-PROTEIN TRANSFERASE FROM FUSIDIUM-GRISEUM

被引：37

作者：

SINGH, SB ^{[1
]}

JONES, ET ^{[1
]}

GOETZ, MA ^{[1
]}

BILLS, GF ^{[1
]}

NALLINOMSTEAD, M ^{[1
]}

JENKINS, RG ^{[1
]}

LINGHAM, RB ^{[1
]}

SILVERMAN, KC ^{[1
]}

GIBBS, JB ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD,RES LABS,W POINT,PA 19486

来源：

TETRAHEDRON LETTERS | 1994年 / 35卷 / 27期

关键词：

D O I：

10.1016/S0040-4039(00)76943-7

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Ras (p21) protein is frequently found mutated in human cancers and must be farnesylated by farnesyl protein-transferase (FPTase) to achieve cell-transforming activity. Our continued search for inhibitors of FPTase as potential cancer chemotherapeutics led to the isolation of fusidienol from extracts of the fungus Fusidium griseum. Fusidienol is a novel and potent oxygen-containing [7/6/6] tricyclic heterocycle.

引用

页码：4693 / 4696

页数：4

共 22 条

[1] RAS GENES
BARBACID, M
[J]. ANNUAL REVIEW OF BIOCHEMISTRY, 1987, 56 : 779 - 827
[2] Barron GL, 1968, SOIL SCI, V106, P477, DOI 10.1097/00010694-196812000-00019
[3] DER CJ, 1991, CANCER CELL-MON REV, V3, P331
[4] Ellis M.B., 1985, MICROFUNGI LAND PLAN
[5] Gibbs J B, 1992, Semin Cancer Biol, V3, P383
[6] RAS C-TERMINAL PROCESSING ENZYMES - MINIREVIEW NEW DRUG TARGETS
GIBBS, JB
[J]. CELL, 1991, 65 (01) : 1 - 4
[7] GIBBS JB, 1993, J BIOL CHEM, V268, P7617
[8] IDENTIFICATION OF RAS FARNESYLTRANSFERASE INHIBITORS BY MICROBIAL SCREENING
HARA, M
AKASAKA, K
AKINAGA, S
OKABE, M
NAKANO, H
GOMEZ, R
WOOD, D
UH, M
TAMANOI, F
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1993, 90 (06) : 2281 - 2285
[9] BENZODIAZEPINE PEPTIDOMIMETICS - POTENT INHIBITORS OF RAS FARNESYLATION IN ANIMAL-CELLS
JAMES, GL
GOLDSTEIN, JL
BROWN, MS
RAWSON, TE
SOMERS, TC
MCDOWELL, RS
CROWLEY, CW
LUCAS, BK
LEVINSON, AD
MARSTERS, JC
[J]. SCIENCE, 1993, 260 (5116) : 1937 - 1942
[10] SELECTIVE-INHIBITION OF RAS-DEPENDENT TRANSFORMATION BY A FARNESYLTRANSFERASE INHIBITOR
KOHL, NE
MOSSER, SD
DESOLMS, SJ
GIULIANI, EA
POMPLIANO, DL
GRAHAM, SL
SMITH, RL
SCOLNICK, EM
OLIFF, A
GIBBS, JB
[J]. SCIENCE, 1993, 260 (5116) : 1934 - 1937

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