期刊
JOURNAL OF CARBOHYDRATE CHEMISTRY
卷 38, 期 3, 页码 167-178出版社
TAYLOR & FRANCIS INC
DOI: 10.1080/07328303.2019.1609021
关键词
Exenatide; sortase A; rhamnose; conjugate
资金
- National Natural Science Foundation of China [21472070, 21602084]
- 111 Project [111-2-06]
- China Postdoctoral Science Foundation [2018M632227]
- Collaborative Innovation Center of Jiangsu Modern Industrial Fermentation
- KLCCB [KLCCB-KF201804]
Exenatide modified with rhamnose as a hapten was designed and synthesized by Sortase A-mediated ligation. An Exenatide peptide analog comprised of 46 amino acids, including the sortase A recognition motif LPETG at the C-terminus, was synthesized by solid phase peptide synthesis method. A tri-glycine modified-rhamnose derivative was chemically synthesized in seven steps in good yield. The site-specific conjugation between them catalyzed by Sortase A completed in 3 h and the rhamnose-modified Exenatide conjugate was obtained after semi-preparative HPLC purification and characterized by MALDI-TOF MS. This method should be generally useful for the synthesis of other Exenatide analog for biological studies. [GRAPHICS] .
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