ROTTLERIN, A NOVEL PROTEIN-KINASE INHIBITOR
ROTTLERIN, A NOVEL PROTEIN-KINASE INHIBITOR
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DOI：
10.1006/bbrc.1994.1199
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发表时间：
1994-02-28
影响因子：
3.1
通讯作者：
MARKS, F
中科院分区：
文献类型：
--
作者：
GSCHWENDT, M;MULLER, HJ;MARKS, F
Rottlerin是一种来自菲律宾野桐的化合物，显示出对PKC具有一定特异性的蛋白激酶抑制作用。在某种程度上，该新型抑制剂能够区分PKC同工酶，PKC δ的IC 50值为3-6 μ M，PKC α、β、γ的IC 50值为30-42 μ M，PKC β、eta、zeta的IC 50值为80-100 μ M。PKC的抑制似乎，至少部分，是由于rottlerin和ATP之间的竞争。在测试的蛋白激酶中，只有CaM-激酶m被rottlerin抑制得与PKC δ一样有效。rottlerin的化学结构可能作为开发新型抑制剂的基础，该抑制剂对不同的PKC同工酶（如PKC δ）或CaM激酶III具有更高的选择性。(C)1994年出版社出版。
Rottlerin, a compound from Mallotus philippinensis, is shown to inhibit protein kinases with some specificity for PKC. To some extent, the novel inhibitor is able to differentiate between PKC isoenzymes, with IC50 values for PKC delta of 3-6 mu M, PKC alpha,beta,gamma of 30-42 mu M and PKC epsilon,eta,zeta of 80-100 mu M. Inhibition of PKC appears, at least in part, to be due to a competition between rottlerin and ATP. Among the protein kinases tested, only CaM-kinase m is suppressed by rottlerin as effectively as PKC delta. The chemical structure of rottlerin might serve as a basis for the development of novel inhibitors with improved selectivity for a distinct PKC isoenzyme, such as PKC delta, or for CaM-kinase III. (C) 1994 Academic Press, Inc.