Enzastaurin hydrochloride.: Protein kinase C β inhibitor, antiangiogenic agent

被引：9
|
作者：
Sorbera, L. A. [1 ]
Serradell, N. [1 ]
Bolos, J. [1 ]
Rosa, E. [1 ]
机构：
[1] Prous Sci, Barcelona 08080, Spain
来源：
DRUGS OF THE FUTURE | 2007年 / 32卷 / 04期
关键词：
D O I：
10.1358/dof.2007.032.04.1095514
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Protein kinase C (PKC) overexpression has been linked to several types of cancer, with the PKC beta isoform suspected to be involved in vascular endothelial growth factor (VEGF)-induced tumor development and angiogenesis and in the apoptosis-regulating phosphatidylinositol 3-kinase (PI3K)/Akt pathway. Targeting of PKC beta therefore represents a potentially effective strategy for the treatment of cancer. Enzastaurin (LY-317615) is an acyclic bisindolylmaleimide that potently and selectively inhibits the PKC beta isoform. Enzastaurin displayed anticancer efficacy in several preclinical cancer models and in clinical trials in patients with advanced cancers. It is currently undergoing phase III development for relapsed glioblastoma multiforme and diffuse B-cell lymphoma.
引用
收藏
页码：297 / 309
页数：13
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