A NEW INHIBITOR OF PROTEIN KINASE-C, RK-286C (4'-DEMETHYLAMINO-4'-HYDROXYSTAUROSPORINE) .1. SCREENING, TAXONOMY, FERMENTATION AND BIOLOGICAL-ACTIVITY

被引：37

作者：

OSADA, H ^{[1
]}

TAKAHASHI, H ^{[1
]}

TSUNODA, K ^{[1
]}

KUSAKABE, H ^{[1
]}

ISONO, K ^{[1
]}

机构：

[1] INST PHYS & CHEM RES, ANTIBIOT LAB, WAKO, SAITAMA 35101, JAPAN

来源：

JOURNAL OF ANTIBIOTICS | 1990年 / 43卷 / 02期

关键词：

D O I：

10.7164/antibiotics.43.163

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

In the course of our screening program using a bleb-forming assay, a new inhibitor of protein kinase C (PKC) was found in the fermentation of a streptomycete. The inhibitor, RK-286C (4′-demethylamino-4′-hydroxystaurosporine), inhibited the morphological change of K 562 cells, a human chronic erythroleukemia cell, induced by phorbol 12, 13-dibutylate at the concentration of 3 μM. The same concentration of the compound inhibited the activity of PKC in vitro and the aggregation of rabbit platelets induced by collagen and arachidonic acid. © 1990, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.

引用

页码：163 / 167

页数：5

共 18 条

[1] RAPID DIFFERENTIATION BETWEEN NOCARDIA + STREPTOMYCES BY PAPER CHROMATOGRAPHY OF WHOLE-CELL HYDROLYSATES [J].

BECKER, B ;

GORDON, RE ;

LECHEVALIER, HA ;

LECHEVALIER, MP .

APPLIED MICROBIOLOGY, 1964, 12 (05) :421-+

[2]

CASTAGNA M, 1982, J BIOL CHEM, V257, P7847

[3] K-252A, A POTENT INHIBITOR OF PROTEIN-KINASE-C FROM MICROBIAL ORIGIN [J].

KASE, H ;

IWAHASHI, K ;

MATSUDA, Y .

JOURNAL OF ANTIBIOTICS, 1986, 39 (08) :1059-1065

[4]

LECHEVALIER M P, 1970, International Journal of Systematic Bacteriology, V20, P435

[5]

LECHEVALIER MP, 1976, BIOL ACTINOMYCETES R, V11, P78

[6] INDUCTION OF MORPHOLOGICAL CHANGE OF HUMAN MYELOID-LEUKEMIA AND ACTIVATION OF PROTEIN-KINASE C BY A NOVEL ANTIBIOTIC, TAUTOMYCIN [J].

MAGAE, J ;

WATANABE, C ;

OSADA, H ;

CHENG, XC ;

ISONO, K .

JOURNAL OF ANTIBIOTICS, 1988, 41 (07) :932-937

[7] PHORBOL DIESTER RECEPTOR CO-PURIFIES WITH PROTEIN KINASE-C [J].

NIEDEL, JE ;

KUHN, LJ ;

VANDENBARK, GR .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES, 1983, 80 (01) :36-40

[8] TURNOVER OF INOSITOL PHOSPHOLIPIDS AND SIGNAL TRANSDUCTION [J].

NISHIZUKA, Y .

SCIENCE, 1984, 225 (4668) :1365-1370

[9] THE ROLE OF PROTEIN KINASE-C IN CELL-SURFACE SIGNAL TRANSDUCTION AND TUMOR PROMOTION [J].

NISHIZUKA, Y .

NATURE, 1984, 308 (5961) :693-698

[10] NEW ALKALOID AM-2282 OF STREPTOMYCES ORIGIN TAXONOMY, FERMENTATION, ISOLATION AND PRELIMINARY CHARACTERIZATION [J].

OMURA, S ;

IWAI, Y ;

HIRANO, A ;

NAKAGAWA, A ;

AWAYA, J ;

TSUCHIYA, H ;

TAKAHASHI, Y ;

MASUMA, R .

JOURNAL OF ANTIBIOTICS, 1977, 30 (04) :275-282

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