Strategy for the development of AdipoR agonists in the treatment of obesity-linked diseases such as type 2 diabetes. AdipoR1 and AdipoR2 were identified in 2003 and were shown to represent key drug targets in obesity-linked diseases. Of the small-molecule AdipoR-targeted compounds, AdipoRon, was reported in 2013, and the crystal structures of AdipoRs (© Protein Data Bank Japan [PDBj] licensed under CC-BY-4.0 International) were determined in 2015. Elucidation of the crystal structures of AdipoRon-AdipoR complexes should prove crucial for the development of first- and best-in-class drugs for type 2 diabetes and obesity-linked diseases [18, 19, 35, 41, 51]