TY  - JOUR
AU  - He Min
AU  - Guan Ni
AU  - Gao Wei-wei
AU  - Liu Qing
AU  - Wu Xiao-yan
AU  - Ma Da-wei
AU  - Zhong Da-fang
AU  - Ge Guang-bo
AU  - Li Chuan
AU  - Chen Xiao-yan
AU  - Yang Ling
AU  - Liao Jia-yu
AU  - Wang Ming-wei
PY  - 2016
TI  - A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with  in vivo  activities
JF  - Acta Pharmacologica Sinica; Vol 33, No 2 (February 2012): Acta Pharmacologica Sinica (Special Feature:Obesity)
Y2  - 2016
KW  - 
N2  - 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.
UR  - http://www.chinaphar.com/article/view/5939