Controlling Receptor Function From The Extracellular Vestibule Of G-Protein Coupled Receptors
CHEMICAL COMMUNICATIONS(2020)
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.
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Key words
extracellular vestibule,receptors,receptor function,g-protein
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