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Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation

Author

Listed:
  • Jang Hyun Choi

    (Harvard Medical School)

  • Alexander S. Banks

    (Harvard Medical School)

  • Theodore M. Kamenecka

    (Translational Research Institute, The Scripps Research Institute, Scripps Florida
    The Scripps Research Molecular Screening Center (SRMSC), The Scripps Research Institute, Scripps Florida)

  • Scott A. Busby

    (The Scripps Research Institute, Scripps Florida)

  • Michael J. Chalmers

    (The Scripps Research Institute, Scripps Florida)

  • Naresh Kumar

    (The Scripps Research Institute, Scripps Florida)

  • Dana S. Kuruvilla

    (The Scripps Research Institute, Scripps Florida)

  • Youseung Shin

    (Translational Research Institute, The Scripps Research Institute, Scripps Florida)

  • Yuanjun He

    (Translational Research Institute, The Scripps Research Institute, Scripps Florida)

  • John B. Bruning

    (Texas A&M University)

  • David P. Marciano

    (The Scripps Research Institute, Scripps Florida)

  • Michael D. Cameron

    (Translational Research Institute, The Scripps Research Institute, Scripps Florida
    The Scripps Research Institute, Scripps Florida
    The Scripps Research Molecular Screening Center (SRMSC), The Scripps Research Institute, Scripps Florida)

  • Dina Laznik

    (Harvard Medical School)

  • Michael J. Jurczak

    (Howard Hughes Medical Institute, Yale University School of Medicine)

  • Stephan C. Schürer

    (Center for Computational Science, University of Miami)

  • Dušica Vidović

    (Center for Computational Science, University of Miami)

  • Gerald I. Shulman

    (Howard Hughes Medical Institute, Yale University School of Medicine)

  • Bruce M. Spiegelman

    (Harvard Medical School)

  • Patrick R. Griffin

    (Translational Research Institute, The Scripps Research Institute, Scripps Florida
    The Scripps Research Institute, Scripps Florida
    The Scripps Research Molecular Screening Center (SRMSC), The Scripps Research Institute, Scripps Florida)

Abstract

Towards better antidiabetic drugs The nuclear receptor PPARγ is the target of thiazolidinedione antidiabetics including rosiglitazone and pioglitazone. These full PPARγ agonists are effective and well tolerated in most patients, but cause fluid retention and weight gain in a minority. In this proof-of-concept study, Choi et al. show the development of specific PPARγ ligands that retain antidiabetic activity through blockade of Cdk5-mediated PPARγ phosphorylation, but that are not full PPARγ agonists. In mouse models, these ligands do not cause the side effects sometimes associated with full PPARγ agonists.

Suggested Citation

  • Jang Hyun Choi & Alexander S. Banks & Theodore M. Kamenecka & Scott A. Busby & Michael J. Chalmers & Naresh Kumar & Dana S. Kuruvilla & Youseung Shin & Yuanjun He & John B. Bruning & David P. Marciano, 2011. "Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation," Nature, Nature, vol. 477(7365), pages 477-481, September.
    • Handle: RePEc:nat:nature:v:477:y:2011:i:7365:d:10.1038_nature10383
    DOI: 10.1038/nature10383
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