Cathepsin B Degradable Peptidic Macromolecules LA-Gly-Phe-Leu-Gly, as a Potential Delivery Vehicle

• 作 者: Xiaomin Zhi Chenjie Fang
• 机 构: School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University
• 出 处: 首都医科大学第四届研究生学术论坛第二分论坛
• 发表日期: 2016年8期
• 关键词: Gly-Phe-Leu-Gly cathepsin B lipoic acid drug delivery linkage

　　Glycine-Phenylalanine-Leucine-Glycine,known as tetrapeptide Gly-Phe-Leu-Gly and can be degraded in the presence of cathepsin B,which is one of the most prominent proteases present in normal cells and tissues according to the recent research.The expression of cathepsin B is greatly increased in human tumors such as prostate,breast,colon,esophageal,gastric,lung,ovarian,thyroid carcinomas,gliomas and melanomas.\So we can exploit the free carboxyl group in Gly-Phe-Leu-Gly to conjugate drugs,and it hydrolysis to release drugs while reaching the tumor cells,this ptovides a controlled way to target drugs to the tumor tissues to a certain extent.Lipoic acid is reported to have very high health care and medical value and can protect thiol enzyme from heavy metal ions.Lipoic acid has applications in stabilization of blood glucose levels,strengthen liver function and elimination of fatigue.Moreover,in comparison to monothiol-ligands,Lipoic acid is bidentate-thiols so that can function as coordinate bonding and strongly modify to the metal materials such as gold,silver,iron et al.So in this study we conjugate lipoic acid with Gly-Phe-Leu-Gly by amide linkage to creat a new compound named as LA-Gly-Phe-Leu-Gly,which can both have the advantages of lipoic and Gly-Phe-Leu-Gly,and may become a potential drug delivery vehicle in future.