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Molecular Pharmacology

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Research ArticleArticle

Discovery of an Ectopic Activation Site on the M1Muscarinic Receptor

Tracy A. Spalding, Carol Trotter, Niels Skjærbæk, Terri L. Messier, Erika A. Currier, Ethan S. Burstein, Donghui Li, Uli Hacksell and Mark R. Brann
Molecular Pharmacology June 2002, 61 (6) 1297-1302; DOI: https://doi.org/10.1124/mol.61.6.1297
Tracy A. Spalding
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Carol Trotter
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Niels Skjærbæk
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Terri L. Messier
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Erika A. Currier
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Ethan S. Burstein
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Donghui Li
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Uli Hacksell
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Mark R. Brann
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Abstract

Receptors have well-conserved regions that are recognized and activated by hormones and neurotransmitters. Most drugs bind to these sites and mimic or block the action of the native ligands. Using a high-throughput functional screen, we identified a potent and selective M1 muscarinic receptor agonist from a novel structural class. Using a series of chimeric receptors, we demonstrated that this ligand activates the receptor through a region that is not conserved among receptor subtypes, explaining its unprecedented selectivity. This region of the receptor is distinct from the conserved region that is recognized by traditional ligands. The finding that receptors for small-molecule transmitters can have multiple, structurally distinct activation sites has broad implications for the study of receptor structure/function and the potential for the discovery of novel ligands with high selectivity.

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Molecular Pharmacology: 61 (6)
Molecular Pharmacology
Vol. 61, Issue 6
1 Jun 2002
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Research ArticleArticle

Discovery of an Ectopic Activation Site on the M1Muscarinic Receptor

Tracy A. Spalding, Carol Trotter, Niels Skjærbæk, Terri L. Messier, Erika A. Currier, Ethan S. Burstein, Donghui Li, Uli Hacksell and Mark R. Brann
Molecular Pharmacology June 1, 2002, 61 (6) 1297-1302; DOI: https://doi.org/10.1124/mol.61.6.1297

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Research ArticleArticle

Discovery of an Ectopic Activation Site on the M1Muscarinic Receptor

Tracy A. Spalding, Carol Trotter, Niels Skjærbæk, Terri L. Messier, Erika A. Currier, Ethan S. Burstein, Donghui Li, Uli Hacksell and Mark R. Brann
Molecular Pharmacology June 1, 2002, 61 (6) 1297-1302; DOI: https://doi.org/10.1124/mol.61.6.1297
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