多靶点药物分子设计

被引:34
作者
郭彦伸
郭宗儒
机构
[1] 中国医学科学院、北京协和医学院药物研究所
关键词
多靶点配体; 药效团组合; 药物分子设计;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100705 [微生物与生化药学];
摘要
作用于单一分子靶标的药物治愈多基因相关疾病如癌症、或影响多个组织或细胞类型的疾病如糖尿病等存在的问题逐渐被人们所认识。与选择性药物的治疗作用相比,几个靶标间的平衡调节能够提供较好的疗效和较低的副作用,同时作用于多个靶标的多靶点药物能够较好地控制复杂的疾病。本文详细比较分析了单靶点药物的不足和多靶点药物的优势,介绍了多靶点配体药物分子设计的方法及需要优化的参数。对于多靶点药物设计,关键的挑战是如何保证获得平衡的活性同时又能够实现选择性以及适当的药代动力学性质。到目前为止,多靶点药物分子设计的方法对于药物化学家、药理学家、毒理学家以及生物化学家仍然是一项新的挑战。
引用
收藏
页码:276 / 281
页数:6
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