文献类型：期刊文献

中文题名：环肽EGFR抑制剂cp-2的合成与体外抗肺癌作用研究

英文题名：Synthesis of cyclopeptide EGFR inhibitor cp-2 and its antitumor activity in vitro

作者：曹河[1];吴君臣[1]

机构：[1]华东理工大学化学与分子工程学院,上海200237

年份：2018

卷号：13

期号：12

起止页码：1367

中文期刊名：中国科技论文

外文期刊名：China Sciencepaper

收录：北大核心:【北大核心2017】；

基金：国家自然科学基金资助项目(21778017)

语种：中文

中文关键词：生物化学;肺癌;表皮生长因子受体(EGFR);环肽抑制剂

外文关键词：biochemistry;lung cancer;epidermal growth factor receptor(EGFR);cyclic peptide inhibitors

摘要：近年来,肺癌的发病率越来越高,对人类健康造成了巨大威胁。针对这一恶性肿瘤,研究在表皮生长因子受体(epidermal growth factor receptor,EGFR)的近膜区选出一段肽序列,并对其进行环化,通过圆二色光谱实验、细胞毒性实验,发现cp-2具有较为稳定的β-折叠结构,对A549、A431细胞的半抑制浓度分别10.13μmol/L和9.71μmol/L,血清稳定性实验还发现cp-2在24h后仍剩余85%。研究表明,cp-2具有较好的肺癌细胞抑制效果及较高的结构稳定性,使得该肽在抗肺癌药物的研究领域具有一定的潜力。
In recent years,the incidence of lung cancer has become higher and higher,posing a great threat to human health.For this malignancy,a peptide sequence was selected in the proximal membrane region of EGFR and circularized.A circularβ-sheet structure was found to be stable for cp-2 by circular dichroism and cytotoxicity experiments has proved that the semi-inhibitory concentrations of A549 and A431 cells are 10.13μmol/L and 9.71μmol/L,respectively.Serum stability experiments also show that cp-2 still remains 85%after 24 hours.cp-2 has a good lung cancer cell inhibitory effect and high structural stability,making the peptide has a certain potential in the field of anti-lung cancer drugs.