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Inhibitory effect of flavonoids on human glutaminyl cyclase.
Li, Manman; Dong, Yao; Yu, Xi; Zou, Yongdong; Zheng, Yizhi; Bu, Xianzhang; Quan, Junmin; He, Zhendan; Wu, Haiqiang.
Afiliación
  • Li M; College of Life Sciences, Shenzhen University, Shenzhen 518060, China; Department of Pharmacy, School of Medicine, Shenzhen University, No. 3688, Nanhai Road, Nanshan, Shenzhen 518060, China.
  • Dong Y; College of Life Sciences, Shenzhen University, Shenzhen 518060, China; Department of Pharmacy, School of Medicine, Shenzhen University, No. 3688, Nanhai Road, Nanshan, Shenzhen 518060, China.
  • Yu X; College of Life Sciences, Shenzhen University, Shenzhen 518060, China; Department of Pharmacy, School of Medicine, Shenzhen University, No. 3688, Nanhai Road, Nanshan, Shenzhen 518060, China.
  • Zou Y; College of Life Sciences, Shenzhen University, Shenzhen 518060, China.
  • Zheng Y; College of Life Sciences, Shenzhen University, Shenzhen 518060, China.
  • Bu X; School of Pharmaceutical Science, Sun Yat-sen University, Guangzhou 510006, China.
  • Quan J; Key Laboratory of Structural Biology, School of Chemical Biology & Biotechnology, Peking University, Shenzhen Graduate School, Shenzhen 518055, China.
  • He Z; Department of Pharmacy, School of Medicine, Shenzhen University, No. 3688, Nanhai Road, Nanshan, Shenzhen 518060, China.
  • Wu H; College of Life Sciences, Shenzhen University, Shenzhen 518060, China; Department of Pharmacy, School of Medicine, Shenzhen University, No. 3688, Nanhai Road, Nanshan, Shenzhen 518060, China. Electronic address: wuhq@szu.edu.cn.
Bioorg Med Chem ; 24(10): 2280-6, 2016 05 15.
Article en En | MEDLINE | ID: mdl-27061673
ABSTRACT
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.
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Flavonoides / Aminoaciltransferasas / Inhibidores Enzimáticos Límite: Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: China
Texto completo
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Texto completo: 1 Banco de datos: MEDLINE Asunto principal: Flavonoides / Aminoaciltransferasas / Inhibidores Enzimáticos Límite: Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: China