Molecular Basis for β-Glucosidase Inhibition by Ring-Modified Calystegine Analogues

Molecular Basis for β-Glucosidase Inhibition by Ring-Modified Calystegine Analogues
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DOI:
10.1002/cbic.200800451
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发表时间:
2008-11-03
期刊:
影响因子:
3.2
通讯作者:
Fernandez, Jose M. Garcia
Fernandez, Jose M. Garcia
中科院分区:
生物学3区
文献类型:
--
作者:
Aguilar, Matilde;Gloster, Tracey M.;Fernandez, Jose M. Garcia

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1-脱氧-6-氧杂-N-(N′-辛基)硫代氨基甲酰基等中性的香花藤碱B2类似物是比天然生物碱更有效的β-葡萄糖苷酶抑制剂。对海栖热袍菌(Thermotoga maritima)GH-A β-葡萄糖苷酶家族的复合物的结构研究表明,该复合物与母体化合物的结合模式明显不同。
Neutral calystegine B2analogues, such as the 1-deoxy-6-oxa-N-(N′-octyl)thiocarbamoyl derivative, proved to be more potent β-glucosidase inhibitors than the natural alkaloid. Structural studies of the complex with a clan GH-A β-glucosidase from Thermotoga maritima showed a binding mode markedly different from that of the parent compound.