Moran Shalev-Benami
Zuckerman Scholar Moran Shalev-Benami, Associate Professor at Weizmann Institute of Science, on the publication of a new study in Science Advances. The study examines how the dopamine D3 receptorrecognizes cariprazine and related molecules. The study creates a framework for understanding the effects different compounds can produce on signaling outcomes, an important step in designing more precise psychiatric medications.
Abstract:
The third-generation antipsychotic cariprazine is a low- efficacy partial agonist of the dopamine D3 receptor (D3R). Here, we report the cryo–electron microscopy structure of cariprazine bound to D3R, establishing a framework for understanding ligand recognition in this receptor. We further determine structures of D3R in complex with a series of cariprazine derivatives spanning inverse agonists to high- efficacy partial agonists.