| Autor: |
Yan Shi, Candy Lee, Peng Sang, Zaid Amso, David Huang, Weixia Zhong, Meng Gu, Lulu Wei, Vân T.B. Nguyen-Tran, Jingyao Zhang, Weijun Shen, Jianfeng Cai |
| Jazyk: |
angličtina |
| Rok vydání: |
2023 |
| Předmět: |
|
| Zdroj: |
Acta Pharmaceutica Sinica B, Vol 13, Iss 4, Pp 1648-1659 (2023) |
| Druh dokumentu: |
article |
| ISSN: |
2211-3835 |
| DOI: |
10.1016/j.apsb.2022.10.014 |
| Popis: |
Peptides are increasingly important resources for biological and therapeutic development, however, their intrinsic susceptibility to proteolytic degradation represents a big hurdle. As a natural agonist for GLP-1R, glucagon-like peptide 1 (GLP-1) is of significant clinical interest for the treatment of type-2 diabetes mellitus, but its in vivo instability and short half-life have largely prevented its therapeutic application. Here, we describe the rational design of a series of α/sulfono-γ-AA peptide hybrid analogues of GLP-1 as the GLP-1R agonists. Certain GLP-1 hybrid analogues exhibited enhanced stability (t1/2 > 14 days) compared to t1/2 ( |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
|
