期刊
ACTA PHARMACOLOGICA SINICA
卷 33, 期 2, 页码 148-154出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/aps.2011.169
关键词
type 2 diabetes; glucagon-like peptide-1; non-peptidic agonist; Boc5; G-protein coupled receptor
资金
- Ministry of Science and Technology of China [2009ZX09302-001, 2012ZX093004011]
- Chinese Academy of Sciences [KSCX1-YW-02-2, KSCX2-YW-R-17]
- Shanghai Science and Technology Development Fund [074319114, 08DZ2291300, 09DZ2291200]
- K C Wong Education Foundation
- CAS
Glucagon-like peptide-1 (GLP-1)-based therapy presents a promising option for treating type 2 diabetes. However, there are several limitations relative to the peptidic GLP-1 mimetics currently on the market or under development. This concern has led to a continued interest in the search for non-peptidic agonists for GLP-1 receptor (GLP-1R). Here, we briefly review the discovery, characterization and current status of a novel class of cyclobutane-derivative-based non-peptidic agonists for GLP-1R, including Boc5 and its newly discovered analogue WB4-24. Although the oral bioavailability of such compounds still poses great challenges, the progress made so far encourages us to identify a truly 'druggable' small molecule agonist for GLP-1R.
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