Inhibitory effect of flavonoids on human glutaminyl cyclase

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• 作者：Manman Li^a ; ^b ; ^&dagger ; ; Yao Dong^a ; ^b ; ^&dagger ; ; Xi Yu^a ; ^b ; Yongdong Zou^a ; Yizhi Zheng^a ; Xianzhang Bu^c ; Junmin Quan^d ; Zhendan He^b ; Haiqiang Wu^a ; ^b ; ^{wuhq@szu.edu.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Glutaminyl cyclase ; Flavonoids ; Synthesis ; Enzyme inhibitor ; Alzheimer&rsquo ; s disease
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2016
• 出版时间：15 May 2016
• 年：2016
• 卷：24
• 期：10
• 页码：2280-2286
• 全文大小：3377 K

文摘

Glutaminyl cyclase (QC) plays an important role in the pathogenesis of Alzheimer’s disease (AD) and can be a potential target for the development of novel anti-AD agents. However, the study of QC inhibitors are still less. Here, phenol-4′ (R1-), C5-OH (R2-) and C7-OH (R3-) modified apigenin derivatives were synthesized as a new class of human QC (hQC) inhibitors. The efficacy investigation of these compounds was performed by spectrophotometric assessment and the structure–activity relationship (SAR) was evaluated. Molecular docking was also carried out to analyze the binding mode of the synthesized flavonoid to the active site of hQC.