芋螺毒素的药物设计学研究进展  

Progress in Study on Drug Design of Conotoxins

作　　者：陈翔[1] 朱永平[1] 

机构地区：[1]浙江大学医学院毒理研究室,浙江杭州310058

出　　处：《药物生物技术》2010年第3期273-277,共5页Pharmaceutical Biotechnology

基　　金：国家重点基础研究发展计划(973计划)项目(2003CB515402);卫生部科学研究基金(浙江省和卫生部共建项目计划)(WKJ2007-2-007)

摘　　要：芋螺毒素(CTX)主要作用于细胞膜上多种离子通道和神经递质/激肽的受体,有很强的生物学活性。CTX结构新颖,功能独特,分子质量小,便于作为分子模式构建和构效关系研究的对象而应用于新药设计。但是其临床给药不方便,吸收率低,稳定性较差,这些缺点也成为药物设计学研究的主要目标。目前已有实验室设计出具有一定活性的CTX类似物,其中一些已经进入临床研究,具有良好的开发和应用的前景。文章从CTX化学修饰优化和计算机辅助设计两个方面对CTX药物设计学研究进展进行综述。The conotoxins have a typical biological activity which modulates the ion channels in cellmembranes and neurotransmitter/bradykinin receptors. Conotoxins have novel structure and unique feature, with low molecular weight, which are easy to be used to build model of the molecular structure-activity relationship studies of new drugs design. However they are incovenient for clinical administration, due to stable and low absorption rate, which has also become one of main objectives of the drug design study. At present, a series of conotoxin analogues with certain activity have been designed and some have been in the stage of clinical study. These studies show that the conotoxins have a good prospect for development and application. The recently published articles on conotoxins drug design and the chemical modification or computer-aided design optimization in CTX drug design are analysed and summarized in the paper.

关 键 词：芋螺毒素 化学修饰 计算机辅助设计 

分 类 号：Q514.3[生物学—生物化学]