%0 Journal Article %T A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities %A He Min %A Guan Ni %A Gao Wei-wei %A Liu Qing %A Wu Xiao-yan %A Ma Da-wei %A Zhong Da-fang %A Ge Guang-bo %A Li Chuan %A Chen Xiao-yan %A Yang Ling %A Liao Jia-yu %A Wang Ming-wei %J Acta Pharmacologica Sinica %D 2016 %B 2016 %9 %! A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities %K %X 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. %U http://www.chinaphar.com/article/view/5939 %V 33 %N 2 %P 148-154 %@ 1745-7254