Peroxisome proliferator-activated receptor gamma (PPARγ) agonists have an outstanding anti-diabetic potential as they promote adipogenesis and lead to the development of small, metabolically healthy adipocytes. However, these molecules also regulate a variety of processes in other cell types. Therefore, the clinical application of some PPARγ agonists is accompanied by serious side effects. To avoid this, Wittrisch et al. developed a peptide drug conjugate with the dual PPARα/γ agonist tesaglitazar (tesa) and a form of neuropeptide Y. This construct binds to NPY1-receptor on adipocytes for cell-type specific uptake. The authors show that the peptide conjugate prevents diabetes progression as efficiently as systemically administered tesa.