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Molecular Pharmacology

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Research ArticleArticle

Small Molecule Allosteric Modulation of the Glucagon-Like Peptide-1 Receptor Enhances the Insulinotropic Effect of Oxyntomodulin

Francis S. Willard, Denise Wootten, Aaron D. Showalter, Emilia E. Savage, James Ficorilli, Thomas B. Farb, Krister Bokvist, Jorge Alsina-Fernandez, Sebastian G. B. Furness, Arthur Christopoulos, Patrick M. Sexton and Kyle W. Sloop
Molecular Pharmacology December 2012, 82 (6) 1066-1073; DOI: https://doi.org/10.1124/mol.112.080432
Francis S. Willard
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Denise Wootten
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Aaron D. Showalter
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Emilia E. Savage
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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James Ficorilli
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Thomas B. Farb
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Krister Bokvist
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Jorge Alsina-Fernandez
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Sebastian G. B. Furness
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Arthur Christopoulos
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Patrick M. Sexton
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Kyle W. Sloop
Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
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Article Information

vol. 82 no. 6 1066-1073
DOI 
https://doi.org/10.1124/mol.112.080432
PubMed 
22930710

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0026-895X
Online ISSN 
1521-0111
History 
  • Received June 8, 2012
  • Accepted August 28, 2012
  • Published online November 14, 2012.

Article Versions

  • Earlier version (August 28, 2012 - 08:14).
  • You are viewing the most recent version of this article.
Copyright & Usage 
Copyright © 2012 The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. Francis S. Willard,
  2. Denise Wootten,
  3. Aaron D. Showalter,
  4. Emilia E. Savage,
  5. James Ficorilli,
  6. Thomas B. Farb,
  7. Krister Bokvist,
  8. Jorge Alsina-Fernandez,
  9. Sebastian G. B. Furness,
  10. Arthur Christopoulos,
  11. Patrick M. Sexton, and
  12. Kyle W. Sloop
  1. Translational Science and Technologies (F.S.W.), Endocrine Discovery (A.D.S., J.F., T.B.F., K.B., K.W.S.), and BioTechnology Discovery Research (J.A.-F.), Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria, Australia (D.W., E.E.S., S.G.B.F., A.C., P.M.S.)
  1. Address correspondence to:
    Dr. Kyle W. Sloop, Endocrine Discovery, Lilly Research Laboratories, Drop Code 0424, Indianapolis, IN 46285. E-mail: sloop_kyle_w{at}lilly.com
  1. F.S.W., D.W., and A.D.S. contributed equally to this work.

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Molecular Pharmacology: 82 (6)
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Research ArticleArticle

Allosteric Modulation of Oxyntomodulin at the GLP-1 Receptor

Francis S. Willard, Denise Wootten, Aaron D. Showalter, Emilia E. Savage, James Ficorilli, Thomas B. Farb, Krister Bokvist, Jorge Alsina-Fernandez, Sebastian G. B. Furness, Arthur Christopoulos, Patrick M. Sexton and Kyle W. Sloop
Molecular Pharmacology December 1, 2012, 82 (6) 1066-1073; DOI: https://doi.org/10.1124/mol.112.080432

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Research ArticleArticle

Allosteric Modulation of Oxyntomodulin at the GLP-1 Receptor

Francis S. Willard, Denise Wootten, Aaron D. Showalter, Emilia E. Savage, James Ficorilli, Thomas B. Farb, Krister Bokvist, Jorge Alsina-Fernandez, Sebastian G. B. Furness, Arthur Christopoulos, Patrick M. Sexton and Kyle W. Sloop
Molecular Pharmacology December 1, 2012, 82 (6) 1066-1073; DOI: https://doi.org/10.1124/mol.112.080432
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