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神经酰胺酶的小分子抑制剂。

Small molecule inhibitors of ceramidases.

作者信息

Saied Essa M, Arenz Christoph

机构信息

Humboldt Universität zu Berlin, Institute for Chemistry, Berlin, Germany.

出版信息

Cell Physiol Biochem. 2014;34(1):197-212. doi: 10.1159/000362995. Epub 2014 Jun 16.

DOI:10.1159/000362995
PMID:24977492
Abstract

The equilibrium between the pro-apoptotic ceramide and pro-vital sphingosine-1-phosphate is considered to be decisive for cell death or survival. The different ceramidases thus play key roles in cell fate and might offer attractive targets for pharmacological intervention. Although until recently only moderately active inhibitors have been described, first in vivo experiments suggest activity against cancer cell survival and multi-drug resistance. Here, we provide a brief overview on the different ceramidases, and we will review the known inhibitors and current strategies for further inhibitor development.

摘要

促凋亡神经酰胺与促生存的1-磷酸鞘氨醇之间的平衡被认为对细胞死亡或存活起决定性作用。因此,不同的神经酰胺酶在细胞命运中发挥关键作用,可能为药物干预提供有吸引力的靶点。尽管直到最近才描述了活性适中的抑制剂,但首次体内实验表明其对癌细胞存活和多药耐药性有活性。在此,我们简要概述不同的神经酰胺酶,并将回顾已知的抑制剂以及进一步开发抑制剂的当前策略。

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