Small molecule allosteric agonists of glucagon-like peptide 1 receptor for treatment of type 2 diabetes

The Glucagon-Like Peptide 1 Receptor (GLP-1R), a member of Class B family of G-protein coupled receptors (GPCRs), is an effective target for the treatment of type-2 diabetes, and its incretin peptide and varied peptide mimetics are adopted drugs. Despite remarkable anti-diabetic effects, GLP-1R peptide-based agonists are limited by several disadvantages. Although considerable progress has been made in developing small molecule, nonpeptide drugs targeting GLP-1R, no small molecule drugs are available currently.

Therefore, novel approaches, such as that developed by Dr. Zhijun Li,in developing small molecule drugs targeting GLP-1R are needed in the treatment of type-2 diabetes.

Dr. Li believes targeting the allosteric sites of GLP-1R for small molecule drug discovery represents a promising alternative for overcoming shortcomings related to GLP-1R peptide-based treatment.

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