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基于蛋白结构的Bcl-2抑制剂设计与开发 被引量：1

Structure-based Design and Development of Bcl-2 Inhibitors
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摘要 Bcl-2家族抗凋亡蛋白的过度表达通常与肿瘤的发生有着密切的关系,而细胞凋亡信号均要经Bcl-2蛋白家族传递。因此,针对Bcl-2家族蛋白的结构特征和功能,设计其特异性抑制剂,以诱导肿瘤细胞凋亡,已成为肿瘤治疗的新策略。综述Bcl-2家族蛋白的结构与功能及其活性位点的分布,介绍基于结构的若干Bcl-2抑制剂的设计与开发。 The over-expression of anti-apoptotic Bcl-2 family proteins is closely associated with the pathogenesis of tumor and the cell apoptosis signals converge on the Bcl-2 protein family.Therefore,the specific Bcl-2 inhibitors designed on the structure features and functions of Bcl-2 family proteins to induce tumor cell apoptosis have displayed a novel strategy for tumor treatment.The structures and functions of Bcl-2 family proteins and their active sites were reviewed.The structure-based design and development of some Bcl-2 inhibitors were also introduced.
作者 张鸣鸣 尤启冬
机构地区 中国药科大学药物化学教研室
出处 《药学进展》 CAS 2010年第7期289-297,共9页 Progress in Pharmaceutical Sciences
基金 抗肿瘤及糖尿病等药物研究与开发技术体系建设"重大新药创制"科技重大专项(No.2008ZX09401-001) 针对重大疾病的先导化合物结构优化设计的关键技术研究"重大新药创制"科技重大专项(No.2009ZX09501-003)
关键词 Bcl-2蛋白家族 小分子Bcl-2抑制剂 基于结构的设计 活性位点 细胞凋亡 肿瘤治疗 Bcl-2 protein family small molecular Bcl-2 inhibitor structure-based design active site cell apoptosis tumor treatment
分类号 R91 [医药卫生—药学]
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参考文献40

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同被引文献12

  • 1Jignesh M, Doshi, Tian DF, et al. Structure - activity relationship studies of ethyl 2 - amino - 6 - bromo - 4 - ( 1 - cyano - 2 - ethoxy - 2 - oxoethyl) - 4H - chromene - 3 - carboxylate ( HA -14 - 1 ), an antagonist for anti - apoptotic Bcl - 2 proteins to overcome drug resistance in cancer [ J ]. J Med Chem, 2006,49 (26) : 773l -7739.
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药学进展
2010年 第7期

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