György M. Keserű

The structure of the dopamine D 3 receptor bound to cariprazine reveals principles for partial agonists with designed pharmacology

The third-generation antipsychotic cariprazine is a low-efficacy partial agonist of the dopamine D 3 receptor (D 3 R). Here, we report the cryo–electron microscopy structure of cariprazine bound to D 3 R, establishing a framework for understanding ligand recognition in this recep...