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Article

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor.

Biochemical pharmacology - 1 Feb 2018

Draper-Joyce Christopher J, Michino Mayako, Verma Ravi Kumar, Klein Herenbrink Carmen, Shonberg Jeremy, Kopinathan Anitha, Scammells Peter J, Capuano Ben, Thal David M, Javitch Jonathan A, Christopoulos Arthur, Shi Lei, Lane J Robert

Abstract excerpt

SB269652 is a negative allosteric modulator of the dopamine D2 receptor (D2R) yet possesses structural similarity to ligands with a competitive mode of interaction. In this study, we aimed to understand the ligand-receptor interactions that confer its allosteric action. We combined site-directed mutagenesis with molecular dynamics simulations using both SB269652 and derivatives from our previous structure...

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Identifiers

PMID: 29325769
DOI: 10.1016/j.bcp.2018.01.002
PMCID: PMC5800995

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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