Discovery of a novel class of negative allosteric modulator of the dopamine D2 receptor through fragmentation of a bitopic ligand

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Discovery of a novel class of negative allosteric modulator of the dopamine D2 receptor through fragmentation of a bitopic ligand

We recently demonstrated that SB269652 (1) engages one protomer of a dopamine D2 receptor (D2R) dimer in a bitopic mode to allosterically inhibit the binding of dopamine at the other protomer. Herein, we investigate structural deter- minants for allostery, focusing on modifications to three moieties...

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Bibliographic Details
Main Authors:	Mistry, Shailesh N., Shonberg, Jeremy, Draper-Joyce, Christopher J., Klein Herenbrink, Carmen, Michino, Mayako, Shi, Lei, Christopoulos, Arthur, Capuano, Ben, Scammells, Peter J., Lane, J. Robert
Format:	Article
Published:	American Chemical Society 2015
Online Access:	https://eprints.nottingham.ac.uk/30315/

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