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A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities

   
@article{APS5939,
	author = {Min He and Ni Guan and Wei-wei Gao and Qing Liu and Xiao-yan Wu and Da-wei Ma and Da-fang Zhong and Guang-bo Ge and Chuan Li and Xiao-yan Chen and Ling Yang and Jia-yu Liao and Ming-wei Wang},
	title = {A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities},
	journal = {Acta Pharmacologica Sinica},
	volume = {33},
	number = {2},
	year = {2016},
	keywords = {},
	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.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/5939}
}