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Discovery of a true bivalent dopamine D2 receptor agonist.

Abstract：

:Employing two different alkyne-modified dopamine agonists to construct bivalent compounds via click chemistry resulted in the identification of a bivalent ligand (11c) for dopamine D2 receptor homodimer, which, compared to its parent monomeric alkyne, showed a 16-fold higher binding affinity for the dopamine D2 receptor and a 5-fold higher potency in a cAMP assay in HEK 293T cells stably expressing D2R. Molecular modeling revealed that 11c can indeed bridge the orthosteric binding sites of a D2R homodimer in a relaxed conformation via the TM5-TM6 interface and allows to largely rationalize the results of the receptor assays.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Qian M,Ricarte A,Wouters E,Dalton JAR,Risseeuw MDP,Giraldo J,Van Calenbergh S

doi

10.1016/j.ejmech.2020.113151

subject

Has Abstract

pub_date

2021-01-04 00:00:00

pages

113151

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(20)31123-5

journal_volume

212

pub_type

杂志文章

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