Issue 91, 2020

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

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

Supplementary files

Article information

Article type
Communication
Submitted
13 Aug 2020
Accepted
13 Oct 2020
First published
13 Oct 2020
This article is Open Access
Creative Commons BY-NC license

Chem. Commun., 2020,56, 14167-14170

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, 56, 14167 DOI: 10.1039/D0CC05532H

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