Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C
Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C
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DOI：
10.1016/j.bmcl.2004.02.097
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发表时间：
2004-06-07
影响因子：
2.7
通讯作者：
Sodeoka, M
中科院分区：
文献类型：
--
作者：
Baba, Y;Ogoshi, Y;Sodeoka, M
蛋白激酶C（Protein Kinase C，PKC）是一个在细胞内信号转导中起重要作用的酶家族。我们已经设计了新的PKC配体具有isobenzofuranone模板，基于建议的相互作用的DAG（1，2-diacyl-sn-glycerol）与PKC δ C1 B配体结合域。合成了几种异苯并呋喃酮衍生物，并评价了它们的PKCalpha结合活性。新戊酰基衍生物1f被认为是一个强大的PKCalpha配体，和构效关系很好地解释了我们提出的结合模型。(C)2004 Elsevier Ltd.保留所有权利。
Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. We have designed novel PKC ligands having an isobenzofuranone template, based on the proposed interaction of DAG (1,2-diacyl-sn-glycerol) with the PKCdelta C1B ligand-binding domain. Several isobenzofuranone derivatives were synthesized and their PKCalpha binding activities were evaluated. The pivaloyl derivative 1f was found to be a strong PKCalpha ligand, and the structure-activity relationship is well explained by our proposed binding model. (C) 2004 Elsevier Ltd. All rights reserved.