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Controlling receptor function from the extracellular vestibule of G-protein coupled receptors

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Abstract

Receptor function is traditionally controlled from the orthosteric binding site of G-protein coupled receptors. Here, we show that the functional activity and signalling of human dopamine D2 and D3 receptor ligands can be fine-tuned from the extracellular secondary binding pocket (SBP) located far from the signalling interface suggesting optimization of the SBP binding part of bitopic ligands might be a useful strategy to develop GPCR ligands with designed functional and signalling profile.

Graphical abstract: Controlling receptor function from the extracellular vestibule of G-protein coupled receptors

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Article information


Submitted
13 Aug 2020
Accepted
13 Oct 2020
First published
13 Oct 2020

This article is Open Access

Chem. Commun., 2020, Advance Article
Article type
Communication

Controlling receptor function from the extracellular vestibule of G-protein coupled receptors

A. Egyed, K. Domány-Kovács, B. Koványi, F. Horti, D. Kurkó, D. J. Kiss, G. Pándy-Szekeres, I. Greiner and G. M. Keserű, Chem. Commun., 2020, Advance Article , DOI: 10.1039/D0CC05532H

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