Small Molecule Inhibitors Targeting Biosynthesis of Ceramide, the Central Hub of the Sphingolipid Network.
Small Molecule Inhibitors Targeting Biosynthesis of Ceramide, the Central Hub of the Sphingolipid Network.
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DOI：
10.1021/acs.jmedchem.0c01664
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发表时间：
2021-01-14
影响因子：
7.3
通讯作者：
Tsukamoto T
中科院分区：
文献类型：
--
作者：
Skácel J;Slusher BS;Tsukamoto T
神经酰胺是由鞘氨酸和由酰胺连接的单一脂肪酸组成的。神经酰胺作为一类主要的生物活性脂质，其上下游代谢产物与癌症、神经变性、糖尿病、微生物发病、肥胖和炎症等多种病理疾病有关。因此，巨大的努力已经致力于破译神经酰胺生物合成中涉及的代谢途径的动力学。鉴于几种不同的酶可以产生神经酰胺，根据潜在的疾病机制，不同的酶靶点已经被追求。本综述的主要目的是从药物化学的角度全面概述迄今为止报道的这些神经酰胺产生酶的小分子抑制剂。
Ceramides are composed of a sphingosine and a single fatty acid connected by an amide linkage. As one of the major classes of biologically active lipids, ceramides and their upstream and downstream metabolites have been implicated in several pathological conditions including cancer, neurodegeneration, diabetes, microbial pathogenesis, obesity, and inflammation. Consequently, tremendous efforts have been devoted to deciphering the dynamics of metabolic pathways involved in ceramide biosynthesis. Given that several distinct enzymes can produce ceramide, different enzyme targets have been pursued depending on the underlying disease mechanism. The main objective of this review is to provide a comprehensive overview of small molecule inhibitors reported to date for each of these ceramide-producing enzymes from a medicinal chemistry perspective.
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