含SPXX序列肽的设计合成及抑菌抗肿瘤活性研究  

Design and Synthesis of Antibacterial and Antitumor Peptides Containing a SPXX Motif

作　　者：郝岩 张若蘅 李崇熙[1] 徐筱杰[1] 

机构地区：[1]北京大学化学与分子工程学院

出　　处：《北京大学学报（自然科学版）》1995年第6期703-710,共8页Acta Scientiarum Naturalium Universitatis Pekinensis

基　　金：国家科委攀登计划项目

摘　　要：根据纺锤霉素（Ｎｅｔｒｏｐｓｉｎ）的晶体结构及与ＤＮＡ作用方式，我们设计合成了３个含ＳＰＸＸ序列的十肽，它们在空间构象上与纺锤霉素类似。应用Ｃｈｏｕ＆Ｆａｓｍａｎ蛋白质二级结构预测方法，推测３个肽应具有β－ｔｕｒｎ结构。３个肽的ＣＤ谱也证实了这一点。通过测定小牛胸腺ＤＮＡ及加入不同量肽后的ＣＤ谱，表明３个肽可与ＤＮＡ结合。实验证明３个肽具有抑菌抗肿瘤活性。这为以后设计选择性识别并结合ＤＮＡ的多肽类药物提供了依据。On the basis of crystal structure and the interaction with DNA of Netro-psin , three 10 residues SPXX motif peptides were designed and synthesized. These structures are similiar to Netropsin’s. The secondary structures of these peptides have been studied by circular dichroism spectra, which satisfy the criteria of β-turn consistent with those obtained by Chou &Fasman prediction method. Circular dichroism of DNA of calf thymus with diffrent quantities of these peptides reveal that they can bind to DNA.These peptides have antibacterial and antitumor activities.

关 键 词：纺锤霉素 抗肿瘤活性 肽 晶体结构 合成 

分 类 号：TQ464.7[化学工程—制药化工]