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Article

Molecular Basis of Ligand Dissociation from the Adenosine A2A Receptor.

Molecular pharmacology - 1 May 2016

Guo Dong, Pan Albert C, Dror Ron O, Mocking Tamara, Liu Rongfang, Heitman Laura H, Shaw David E, IJzerman Adriaan P

Abstract excerpt

How drugs dissociate from their targets is largely unknown. We investigated the molecular basis of this process in the adenosine A2Areceptor (A2AR), a prototypical G protein-coupled receptor (GPCR). Through kinetic radioligand binding experiments, we characterized mutant receptors selected based on molecular dynamic simulations of the antagonist ZM241385 dissociating from the A2AR. We discovered mutations that...

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PMID: 26873858
DOI: 10.1124/mol.115.102657

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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