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...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Published: |
American Chemical Society
2015
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| Online Access: | https://eprints.nottingham.ac.uk/30315/ |