2:03 PM
Nov 02, 2017
 |  BC Innovations  |  Translation in Brief

A new pocket for D4

Crystal structure paves way to dopamine D4 receptor-selective agonists

The early promise of the dopamine D4 receptor as a therapeutic target for psychiatric disorders hasn’t been borne out because of the difficulty of producing sufficiently selective compounds. Last month in Science, a collaboration between UNC Chapel Hill and UCSF united crystallography and in silico drug discovery to find a selective D4 agonist that could spur new cognitive therapies.

The study was led by Bryan Roth, a pharmacology professor at University of North Carolina at Chapel Hill, and Brian Shoichet, a pharmacy professor at the University of California San Francisco, who teamed up to use Roth’s expertise in protein expression and crystallography and Shoichet’s in silico drug screening expertise.

The history of dopamine receptors is littered with failed attempts to crystallize the proteins, which belong to the family of G-protein coupled receptors (GPCRs). But the duo reasoned that Roth’s access to the Advanced Photon Source at a Department of...

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