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- Title
A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities.
- Authors
He, Min; Guan, Ni; Gao, Wei-wei; Liu, Qing; Wu, Xiao-yan; Ma, Da-wei; Zhong, Da-fang; Ge, Guang-bo; Li, Chuan; Chen, Xiao-yan; Yang, Ling; Liao, Jia-yu; Wang, Ming-wei
- Abstract
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.
- Subjects
TYPE 2 diabetes treatment; GLUCAGON-like peptide 1; GLUCAGON-like peptide-1 receptor; DRUG bioavailability; CYCLOBUTANE; ORAL drug administration; MEDICAL protocols; THERAPEUTICS
- Publication
Acta Pharmacologica Sinica, 2012, Vol 33, Issue 2, p148
- ISSN
1671-4083
- Publication type
Article
- DOI
10.1038/aps.2011.169