文章摘要
刘振,李福星,万升标.共价药物靶蛋白活性结合位点研究综述[J].中国海洋药物,2016,35(1):82-93.
共价药物靶蛋白活性结合位点研究综述
Review of active binding sites of covalent drugs
投稿时间:2015-01-30  修订日期:2015-03-30
DOI:
中文关键词: 共价药物  药物设计  靶蛋白  共价结合位点  氨基酸残基
英文关键词: covalent drug  drugdesign  target protein  covalent binding site  amino acid residue.
基金项目:国家自然科学基金项目(面上项目,重点项目,重大项目)
作者单位E-mail
刘振 中国海洋大学医药学院 liuzhen19900616@163.com 
李福星 中国海洋大学医药学院  
万升标 中国海洋大学医药学院  
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中文摘要:
      共价药物以其对靶蛋白的高抑制率而在临床中广泛使用,并逐渐引起药学家的重视。本文总结四种不同类型的共价结合位点,被“酸性氨基酸-碱性氨基酸-丝氨酸/苏氨酸”三元体结构活化的丝氨酸/苏氨酸残基是共价药物的潜在共 价结合位点,活性口袋附近半胱氨酸巯基同样是潜在的亲核基团,这两类氨基酸残基都能共价结合药物中的亲电基团。因此这些活性结合位点的发现是研发共价键药物的关键,尤其适合于具有新骨架和新结构的海洋天然产物的药物研发。
英文摘要:
      Covalent drugs are widely used in clinic for their high inhibition to target proteins, and gradually draw attention pharmacists. This paper summarizes four different types of covalent binding sites, the serine/threonine residue which is activated by “acidic amino acid - alkaline amino acid - serine/threonine” structure is a potential covalent binding site for covalent drugs, the sulfhydryl group on cysteine residue which near target protein's binding pocket is also a potential nucleophilic group. These two specific amino acid residues are most likely covalently binding with the electrophilic groups of covalent drugs. As a result, the discovery of these active binding sites is a key to covalent drug especially for the marine natural product drugs with new frame and new structure research and development.
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