Literature DB >> 18656368

Microwave-assisted solid phase synthesis, PEGylation, and biological activity studies of glucagon-like peptide-1(7-36) amide.

Yushi Chi1, Huibin Zhang, Wenlong Huang, Jinpei Zhou, Yinghong Zhou, Hai Qian, Shuaijian Ni.   

Abstract

The insulinotropic hormone glucagon-like peptide-1 (GLP-1) is rapidly inactivated in the body. In order to improve its stability, we replaced the enzymatic hydrolyzation position Ala(8)with Gly and replaced Ala(30) with Cys firstly. Then the modified peptide was further PEGylated at thiol group of Cys(30). Biological activity studies showed that the resulting mPEG-MAL-Gly(8)-Cys(30)-GLP-1(7-36)-NH(2) exhibited long-lasting effect while maintaining moderate glucose-lowering activity.

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Year:  2008        PMID: 18656368     DOI: 10.1016/j.bmc.2008.07.019

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  2 in total

1.  Novel coumarin modified GLP-1 derivatives with enhanced plasma stability and prolonged in vivo glucose-lowering ability.

Authors:  Jing Han; Lidan Sun; Xun Huang; Zheng Li; Chenyu Zhang; Hai Qian; Wenlong Huang
Journal:  Br J Pharmacol       Date:  2014-09-05       Impact factor: 8.739

2.  Engineering a protease-based and site-specific PEGylation-based strategy for the controlled release of exenatide.

Authors:  Aihong Zhang; Yin Lin; Shirly Nong; Wei Zhao; Mei Dong
Journal:  RSC Adv       Date:  2020-06-30       Impact factor: 4.036

  2 in total

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