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Novel pharmacological applications of G-protein-coupled receptor-G protein fusions (2007)
Journal Article
Milligan, G., Parenty, G., Stoddart, L. A., & Lane, J. R. (2007). Novel pharmacological applications of G-protein-coupled receptor-G protein fusions. Current Opinion in Pharmacology, 7(5), 521-526. https://doi.org/10.1016/j.coph.2007.06.007

Single, bi-functional polypeptides consisting of a G-protein-coupled receptor (GPCR) linked directly to a G protein alpha subunit have been employed for a number of years to study many aspects of signal initiation, including the roles of post-transla... Read More about Novel pharmacological applications of G-protein-coupled receptor-G protein fusions.

Protean agonism at the dopamine D2 receptor: (S)-3-(3-hydroxyphenyl)-N-propylpiperidine is an agonist for activation of Go1 but an antagonist/inverse agonist for Gi1,Gi2, and Gi3 (2007)
Journal Article
Lane, J. R., Powney, B., Wise, A., Rees, S., & Milligan, G. (2007). Protean agonism at the dopamine D2 receptor: (S)-3-(3-hydroxyphenyl)-N-propylpiperidine is an agonist for activation of Go1 but an antagonist/inverse agonist for Gi1,Gi2, and Gi3. Molecular Pharmacology, 71(5), 1349-1359. https://doi.org/10.1124/mol.106.032722

A range of ligands displayed agonism at the long isoform of the human dopamine D(2) receptor, whether using receptor-G protein fusions or membranes of cells in which pertussis toxin-resistant mutants of individual Galpha(i)-family G proteins could be... Read More about Protean agonism at the dopamine D2 receptor: (S)-3-(3-hydroxyphenyl)-N-propylpiperidine is an agonist for activation of Go1 but an antagonist/inverse agonist for Gi1,Gi2, and Gi3.