GLU-GLP-1 DUAL AGONIST SIGNALING-SELECTIVE COMPOUNDS

摘要

The present application relates to methods of screening Glu-GLP1 dual agonists (GGDAs) that activate alternative intracellular signalling pathways through the Glucagon receptor (Glu R). Compounds have been identified as partial agonists rather than full agonists, eliciting a submaximal response, presumably caused by generation of an alternative conformational state of the receptor induced by the ligand-receptor interaction. The compounds may be useful in the treatment of metabolic diseases, e.g., diabetes, obesity, and related glucose metabolism diseases, or other conditions characterized by excess body weight.