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本文引用的文献

1
Inhibitors of protein kinase C. 3. Potent and highly selective bisindolylmaleimides by conformational restriction.蛋白激酶C抑制剂。3. 通过构象限制得到的强效且高选择性的双吲哚马来酰胺类化合物。
J Med Chem. 1993 Jan 8;36(1):21-9. doi: 10.1021/jm00053a003.
2
Activation of the zeta isozyme of protein kinase C by phosphatidylinositol 3,4,5-trisphosphate.磷脂酰肌醇3,4,5-三磷酸对蛋白激酶C的ζ同工酶的激活作用。
J Biol Chem. 1993 Jan 5;268(1):13-6.
3
Protein kinase C contains a pseudosubstrate prototope in its regulatory domain.蛋白激酶C在其调节结构域中含有一个假底物原基。
Science. 1987 Dec 18;238(4834):1726-8. doi: 10.1126/science.3686012.
4
Potent selective inhibitors of protein kinase C.蛋白激酶C的强效选择性抑制剂。
FEBS Lett. 1989 Dec 18;259(1):61-3. doi: 10.1016/0014-5793(89)81494-2.
5
Purification and characterisation of bovine brain protein kinase C isotypes alpha, beta and gamma.牛脑蛋白激酶Cα、β和γ亚型的纯化与鉴定
Eur J Biochem. 1989 Jun 1;182(1):129-37. doi: 10.1111/j.1432-1033.1989.tb14809.x.
6
K252a is a potent and selective inhibitor of phosphorylase kinase.K252a是磷酸化酶激酶的一种强效且选择性抑制剂。
Biochem Biophys Res Commun. 1990 Aug 31;171(1):148-54. doi: 10.1016/0006-291x(90)91369-4.
7
Expression, purification, and characterization of protein kinase C-epsilon.蛋白激酶C-ε的表达、纯化及特性分析
J Biol Chem. 1990 May 5;265(13):7301-7.
8
Expression of protein kinase C isotypes using baculovirus vectors.利用杆状病毒载体表达蛋白激酶C同工型
Methods Enzymol. 1991;200:670-3. doi: 10.1016/0076-6879(91)00179-z.
9
Expression of protein kinase C genes in hemopoietic cells is cell-type- and B cell-differentiation stage specific.蛋白激酶C基因在造血细胞中的表达具有细胞类型和B细胞分化阶段特异性。
J Immunol. 1991 Dec 1;147(11):3981-7.
10
Protein kinase C.蛋白激酶C
Pharmacol Ther. 1991;51(1):71-95. doi: 10.1016/0163-7258(91)90042-k.

双吲哚马来酰亚胺（蛋白激酶C的选择性抑制剂）的同工酶特异性

Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C.

作者信息

Wilkinson S E, Parker P J, Nixon J S

机构信息

Research Centre, Roche Products Ltd., Welwyn Garden City, Herts, U.K.

出版信息

Biochem J. 1993 Sep 1;294 ( Pt 2)(Pt 2):335-7. doi: 10.1042/bj2940335.

DOI:10.1042/bj2940335
PMID:8373348
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1134458/
Abstract

The protein kinase C (PKC) family of isoenzymes is believed to mediate a wide range of signal-transduction pathways in many different cell types. A series of bisindolylmaleimides have been evaluated as inhibitors of members of the conventional PKC family (PKCs-alpha, -beta, -gamma) and of a representative of the new, Ca(2+)-independent, PKC family, PKC-epsilon. In contrast with the indolocarbazole staurosporine, all the bisindolylmaleimides investigated showed slight selectivity for PKC-alpha over the other isoenzymes examined. In addition, bisindolylmaleimides bearing a conformationally restricted side-chain were less active as inhibitors of PKC-epsilon. Most noticeable of these was Ro 32-0432, which showed a 10-fold selectivity for PKC-alpha and a 4-fold selectivity for PKC-beta I over PKC-epsilon.

摘要

蛋白激酶C（PKC）同工酶家族被认为在许多不同细胞类型中介导广泛的信号转导途径。一系列双吲哚马来酰胺已被评估为传统PKC家族成员（PKC-α、-β、-γ）以及新型、不依赖Ca²⁺的PKC家族代表PKC-ε的抑制剂。与吲哚咔唑星形孢菌素不同，所有研究的双吲哚马来酰胺对PKC-α的选择性略高于其他检测的同工酶。此外，带有构象受限侧链的双吲哚马来酰胺作为PKC-ε的抑制剂活性较低。其中最显著的是Ro 32-0432，它对PKC-α的选择性为10倍，对PKC-βI的选择性比对PKC-ε高4倍。