Structural basis of protein kinase C activation by diacylglycerols and tumor promoters.
Structural basis of protein kinase C activation by diacylglycerols and tumor promoters.
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二酰甘油和肿瘤促进剂激活蛋白激酶 C 的结构基础。
DOI：
10.1021/bi00123a001
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发表时间：
1992
期刊：
影响因子：
2.9
通讯作者：
Kishi,Y
中科院分区：
文献类型：
--
作者：
Rando,RR;Kishi,Y
Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115, and Department of Chemistry, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138 Received July 23, 1991; Revised Manuscript Received November 14, 1991 abstract: Protein kinase C is a ubiquitous and important regulatory enzyme. The enzyme is physiologically activated in a temporary manner by (S)-diacylglycerols (DAGs), which are themselves generated by the phospholipase C mediated hydrolysis of polyphosphoinositides. The (S)-DAGs specifically bind to the regulatory domain of PKC and cause the activation of the PKC toward substrate. Minor modifications in the DAG result in inactive molecules. On the other hand, the structurally diverse, polycyclic tumor promoters also specifically activate PKC by binding to the same effector site as do the DAGs. The object of this paper is to present a discrete structural model that accounts for the activation of PKC by both the tumor promoters and the DAGs. The unique model presented is based on experimentation rather than on computer-driven hypotheses which, experience has shown, generally produce incorrect structural models when applied to PKC. The modeldescribed here begins with a structural analysis of the tumor-promoting debromoaplysiatoxins (DATs). DAT is an ideal starting molecule, because it is conformationally rigid with a known relative and absolute configuration, and it is synthetically manipulable. The pharmacophore of
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二酰甘油对蛋白激酶C激活特异性的进一步研究。
DOI：
--
发表时间：
1987
期刊：
Biochemical and Biophysical Research Communications - BBRC
影响因子：
--
作者：
M. Go;K. Sekiguchi;H. Nomura;U. Kikkawa;Y. Nishizuka
通讯作者：
Y. Nishizuka
二酰基甘油的脂肪酰基部分对于钙激活的磷脂依赖性蛋白激酶的激活的特异性。
DOI：
--
发表时间：
1982
期刊：
Journal of Biochemistry (Tokyo)
影响因子：
--
作者：
T. Mori;Y. Takai;B. Yu;J. Takahashi;Y. Nishizuka;T. Fujikura
通讯作者：
T. Fujikura
DOI：
10.1016/s0021-9258(18)34459-4
发表时间：
1982-07
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
M. Castagna;Y. Takai;K. Kaibuchi;K. Sano;U. Kikkawa;Y. Nishizuka
通讯作者：
M. Castagna;Y. Takai;K. Kaibuchi;K. Sano;U. Kikkawa;Y. Nishizuka
DOI：
10.1016/s0021-9258(18)33173-9
发表时间：
1983-01
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Akira Kishimoto;Norio Kajikawag;Makoto Shiotan;Yasutomi Nishizuka
通讯作者：
Akira Kishimoto;Norio Kajikawag;Makoto Shiotan;Yasutomi Nishizuka
肿瘤促进剂的受体模型：teleocidins 和佛波酯的合理叠加。
DOI：
10.1073/pnas.85.11.3688
发表时间：
1988
影响因子：
11.1
作者：
Akiko Itai;Yuichi Kato;N. Tomioka;Yoichi Iitaka;Yasuyuki Endo;Masashi Hasegawa;Koichi Shudo;Hirota Fujiki;Shin
通讯作者：
Shin