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Molecular Pharmacology

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OtherArticle

Michaelis-Menten quantification of ligand signalling bias applied to the promiscuous Vasopressin V2 receptor

Franziska Marie Heydenreich, Bianca Plouffe, Aurelien Rizk, Dalibor Milic, Joris Zhou, Billy Breton, Christian Le Gouill, Asuka Inoue, Michel Bouvier and Dmitry Veprintsev
Molecular Pharmacology July 2, 2022, MOLPHARM-AR-2022-000497; DOI: https://doi.org/10.1124/molpharm.122.000497
Franziska Marie Heydenreich
1Structural Studies, MRC Laboratory of Molecular Biology, United Kingdom
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  • ORCID record for Franziska Marie Heydenreich
  • For correspondence: dmitry.veprintsev@nottingham.ac.uk
Bianca Plouffe
2Wellcome-Wolfson Institute for Experimental Medicine, Queen's University Belfast, United Kingdom
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Aurelien Rizk
3InterAx Biotech AG, Switzerland
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Dalibor Milic
4Department of Structural and Computational Biology, University of Vienna, Austria
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Joris Zhou
5Institute for Research in Immunology and Cancer, University of Montreal, Canada
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Billy Breton
5Institute for Research in Immunology and Cancer, University of Montreal, Canada
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Christian Le Gouill
6University of Montreal, Canada
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Asuka Inoue
7Tohoku University, Japan
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Michel Bouvier
8Department of Biochemistry and Molec ular Medicine, University of Montreal, Canada
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  • For correspondence: dmitry.veprintsev@nottingham.ac.uk
Dmitry Veprintsev
9School of Life Sciences, University of Nottingham, United Kingdom
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  • For correspondence: dmitry.veprintsev@nottingham.ac.uk
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  • Data Supplement

    • Supplemental Figure -

      Supplemental Figure S1. Correlation of the peptide modifications relative to the AVP with their signaling
      properties. A. A heat map showing the logBmm values. B. Observed trends of peptide modification on biased signaling.

    • Supplemental Table -

      Supplemental Table S1. ANOVA, Dunnett’s multiple comparison test and BRET data. Signal amplitudes for each ligand were compared for each biosensor using one-way ANOVA and Dunnett’s multiple comparisons test. Amplitudes (labelled “Emax”) and logEC50s are listed as mean, standard error of the mean (SEM) and number of replicates (N).

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Molecular Pharmacology: 102 (3)
Molecular Pharmacology
Vol. 102, Issue 3
1 Sep 2022
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OtherArticle

Michaelis Menten quantification of GPCR-G protein signalling

Franziska Marie Heydenreich, Bianca Plouffe, Aurelien Rizk, Dalibor Milic, Joris Zhou, Billy Breton, Christian Le Gouill, Asuka Inoue, Michel Bouvier and Dmitry Veprintsev
Molecular Pharmacology July 2, 2022, MOLPHARM-AR-2022-000497; DOI: https://doi.org/10.1124/molpharm.122.000497

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Michaelis Menten quantification of GPCR-G protein signalling

Franziska Marie Heydenreich, Bianca Plouffe, Aurelien Rizk, Dalibor Milic, Joris Zhou, Billy Breton, Christian Le Gouill, Asuka Inoue, Michel Bouvier and Dmitry Veprintsev
Molecular Pharmacology July 2, 2022, MOLPHARM-AR-2022-000497; DOI: https://doi.org/10.1124/molpharm.122.000497
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