BioCentury
ARTICLE | Translation in Brief

A new pocket for D4

Crystal structure paves way to dopamine D4 receptor-selective agonists

November 2, 2017 9:03 PM UTC

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. ...