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考虑醛糖还原酶特性的基于配体的药物设计

Ligand-based drug design considering specific features of aldose reductase
课程网址: http://videolectures.net/biophysics2018_majekova_aldose_reductase...  
主讲教师: Magdalena Majekova
开课单位: 苏黎世大学
开课时间: 2018-07-09
课程语种: 英语
中文简介:
醛糖还原酶是多元醇途径中的限速酶,是葡萄糖毒性的主要机制之一。醛糖还原酶抑制剂有助于预防糖尿病并发症和其他与葡萄糖毒性相关的疾病。醛糖还原酶(EC:1.1.1.21)属于醛糖-酮还原酶超家族,是AR的三维结构,已在许多研究工作中得到探索。醛糖还原酶对许多底物进行催化,如脂醛、甲基乙二醛、脂肪族和芳香族醛、柔红霉素、阿霉素等。除了PGH2转化为PGD2(在没有辅因子NADPH或NADP+的情况下进行)外,AR的所有其他已知催化过程均依赖NADPH。我们对基于配体的药物设计进行了综述,结果发现了有效的抑制剂(1),突出了醛糖还原酶的具体特征。
课程简介: Aldose reductase is as a rate-limiting enzyme in the polyol pathway, one of the main mechanisms of glucose toxicity. Inhibitors of aldose reductase showed to be helpful in prevention of diabetic complications and other disorders connected related to a glucose toxicity. Aldose reductase (EC: 1.1.1.21), the three-dimensional structure of AR has been explored in many research works, belongs to the aldo-keto reductase superfamily. Aldose reductase catalyzes many substrates, as lipid aldehydes, methyl glyoxal, aliphatic and aromatic aldehydes, daunorubicin, doxorubicin, etc. With the exception of PGH2 transformation to PGD2, which proceeds in the absence of cofactors NADPH or NADP + , all other known catalytic processes of AR are NADPH-dependent. We present a survey of ligand-based drug design, which resulted in identification of efficient inhibitors (1), with highlighting the specific features of aldose reductase.  
关 键 词: 醛糖还原酶; 催化; 基于配体
课程来源: 视频讲座网
数据采集: 2021-11-13:zkj
最后编审: 2021-11-13:zkj
阅读次数: 42