Ontology highlight
ABSTRACT:
SUBMITTER: Lane JR
PROVIDER: S-EPMC4138267 | biostudies-literature | 2014 Sep
REPOSITORIES: biostudies-literature
Lane J Robert JR Donthamsetti Prashant P Shonberg Jeremy J Draper-Joyce Christopher J CJ Dentry Samuel S Michino Mayako M Shi Lei L López Laura L Scammells Peter J PJ Capuano Ben B Sexton Patrick M PM Javitch Jonathan A JA Christopoulos Arthur A
Nature chemical biology 20140810 9
SB269652 is to our knowledge the first drug-like allosteric modulator of the dopamine D2 receptor (D2R), but it contains structural features associated with orthosteric D2R antagonists. Using a functional complementation system to control the identity of individual protomers within a dimeric D2R complex, we converted the pharmacology of the interaction between SB269652 and dopamine from allosteric to competitive by impairing ligand binding to one of the protomers, indicating that the allostery r ...[more]