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

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

  • Acta Pharmacol Sin. 2012 Feb;33(2):148-54. doi: 10.1038/aps.2011.169.
Min He 1,  Ni Guan,  Wei-wei Gao,  Qing Liu,  Xiao-yan Wu,  Da-wei Ma,  Da-fang Zhong,  Guang-bo Ge,  Chuan Li,  Xiao-yan Chen,  Ling Yang,  Jia-yu Liao,  Ming-wei Wang
Affiliations

Affiliation

  • 1 National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.
PMID: 22301855 DOI: 10.1038/aps.2011.169
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.

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