张伟, 宋竟婧, 王锐*
( 兰州大学基础医学院,兰州市 730000; )
医学论文发表摘要: 肿瘤的靶向治疗可以显著提高药物的治疗效率。氨肽酶N(CD13)是一种跨膜肽酶,在一些实体瘤和中血管中高表达。NGR序列是氨肽酶的配体,能够通过受体介导的内吞途径进入到细胞内。我们将NGR靶向分子与只具有10个氨基酸的抗菌肽KSL进行连接,合成了一类新型的靶向抗菌肽。我们的研究表明合成的偶联物可以显著杀伤具有CD13高表达细胞,而对正常细胞具有非常低的毒性。
关键词: 肿瘤靶向治疗;抗菌肽;NGR'
ZHANG Wei, SONG jingjing, WANG Rui*
( School of Basic Medical Sciences, Lanzhou University, Lanzhou 730000; )
Abstract: Tumor targeted therapy can significantly improve the theraputic index. Aminopeptidase N (CD13) is a transmembrane ectopeptidase and it is highly expressed on tumors cells and newblood vessels. NGR sequenc is efficient target molecule and can enter cells after binding to the CD13. In this study, we designed and synthesized a novel tumor targeted antimcirobial peptide by conjugation of NGR with KSL, a short antimicrobial peptidewith only 10 amino acids. Our results showed this conjugates could kill cells with highly expressing CD13, while had low toxcity to normal cells.
Keywords: tumor targeted therapy; antimicrobial peptide; NGR
作者简介: 张伟(1979-),男,副教授、硕导,多肽药物化学
通信联系人: 王锐(1963-),男,教授、博导,多肽药物化学
中国科技论文在线:张伟,宋竟婧,王锐. NGR-抗菌肽偶联物的设计及抗肿瘤活性[EB/OL].北京:中国科技论文在线 [2017-04-28]