Synthesis and Biological Characterization of Myristic Acid-Conjugated Thymopentin Analogs
Yuanyan Tan; Wei Wang; Chunlei Wu; Zhengyin Pan; Guiyang Yao; Lijing Fang; Wu Su
2015
会议名称2015年全国药物化学学术会议暨第五届中英药物化学学术会议(CMCS2015)
会议地点Lanzhou, China
英文摘要Controlled release of peptides by plasma albumin is a successful strategy to extend half-life and improve their therapeutic effects. The short plasma half-life of thymopentin (TP5) has dramatically limited its clinical application for immunodeficiency diseases. Herein, a TP5 derivative was prepared by conjugating myristic acid at the C-terminal (TP5-MA). TP5-MA showed well preserved biological characteristics and significant longer elimination half-life in human plasma compared with TP5. Cytotoxicity test revealed that TP5-MA had a relatively low toxicity to spleen lymphocytes. Furthermore, the protracted immunomodulating effect was confirmed by the immunodepression rat model with subcutaneous injections of TP5-MA. It highly enhanced pharmacokinetic and pharmacodynamic properties without significant toxicity at the clinic dosage, expecting to broaden the potential clinical application of TP5-MA
收录类别其他
语种英语
内容类型会议论文
源URL[http://ir.siat.ac.cn:8080/handle/172644/7458]  
专题深圳先进技术研究院_医药所
作者单位2015
推荐引用方式
GB/T 7714
Yuanyan Tan,Wei Wang,Chunlei Wu,et al. Synthesis and Biological Characterization of Myristic Acid-Conjugated Thymopentin Analogs[C]. 见:2015年全国药物化学学术会议暨第五届中英药物化学学术会议(CMCS2015). Lanzhou, China.
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