Skip to main content
Advertisement

Main menu

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET

User menu

  • My alerts
  • Log in
  • My Cart

Search

  • Advanced search
Molecular Pharmacology
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET
  • My alerts
  • Log in
  • My Cart
Molecular Pharmacology

Advanced Search

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Special Sections
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Submit
  • Visit molpharm on Facebook
  • Follow molpharm on Twitter
  • Follow molpharm on LinkedIn
Research ArticleArticle

In Vivo Imaging Reveals Selective Peroxisome Proliferator Activated Receptor Modulator Activity of the Synthetic Ligand 3-(1-(4-Chlorobenzyl)-3-t-butylthio-5-isopropylindol-2-yl)-2,2-dimethylpropanoic acid (MK-886)

Andrea Biserni, Fabio Giannessi, Anna Floriana Sciarroni, Ferdinando Maria Milazzo, Adriana Maggi and Paolo Ciana
Molecular Pharmacology May 2008, 73 (5) 1434-1443; DOI: https://doi.org/10.1124/mol.107.042689
Andrea Biserni
Department of Pharmacological Sciences, Center of Excellence on Neurodegenerative Diseases, University of Milan, Milan, Italy (A.B., P.C., A.M.); Transgenic Operative Products s.r.l., Lodi, Italy (A.B.); and Department of Endocrinology and Metabolism, Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Pomezia, Italy (F.G., A.F.S., F.M.M.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Fabio Giannessi
Department of Pharmacological Sciences, Center of Excellence on Neurodegenerative Diseases, University of Milan, Milan, Italy (A.B., P.C., A.M.); Transgenic Operative Products s.r.l., Lodi, Italy (A.B.); and Department of Endocrinology and Metabolism, Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Pomezia, Italy (F.G., A.F.S., F.M.M.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Anna Floriana Sciarroni
Department of Pharmacological Sciences, Center of Excellence on Neurodegenerative Diseases, University of Milan, Milan, Italy (A.B., P.C., A.M.); Transgenic Operative Products s.r.l., Lodi, Italy (A.B.); and Department of Endocrinology and Metabolism, Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Pomezia, Italy (F.G., A.F.S., F.M.M.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Ferdinando Maria Milazzo
Department of Pharmacological Sciences, Center of Excellence on Neurodegenerative Diseases, University of Milan, Milan, Italy (A.B., P.C., A.M.); Transgenic Operative Products s.r.l., Lodi, Italy (A.B.); and Department of Endocrinology and Metabolism, Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Pomezia, Italy (F.G., A.F.S., F.M.M.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Adriana Maggi
Department of Pharmacological Sciences, Center of Excellence on Neurodegenerative Diseases, University of Milan, Milan, Italy (A.B., P.C., A.M.); Transgenic Operative Products s.r.l., Lodi, Italy (A.B.); and Department of Endocrinology and Metabolism, Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Pomezia, Italy (F.G., A.F.S., F.M.M.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Paolo Ciana
Department of Pharmacological Sciences, Center of Excellence on Neurodegenerative Diseases, University of Milan, Milan, Italy (A.B., P.C., A.M.); Transgenic Operative Products s.r.l., Lodi, Italy (A.B.); and Department of Endocrinology and Metabolism, Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Pomezia, Italy (F.G., A.F.S., F.M.M.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF
Loading

Abstract

We report here the finding of a new pharmacological activity of a well known antagonist of peroxisome proliferator-activated receptors (PPARs). PPARs belong to the family of nuclear receptors playing a relevant role in mammalian physiology and are currently believed to represent a major target for the development of innovative drugs for metabolic and inflammatory diseases. In the present study, the application of reporter animal technology was instrumental to obtain the global pharmacological profiling indispensable to unraveling 3-(1-(4-chlorobenzyl)-3-t-butylthio-5-isopropylindol-2-yl)-2,2-dimethylpropanoic acid (MK-886)-selective PPAR modulator (SPPARM) activity not underlined by previous traditional, cell-based studies. The results of this study, demonstrating the usefulness of reporter mice, may open new avenues for the development of innovative drugs for cardiovascular, endocrine, neural, and skeletal systems characterized by limited side effects.

  • The American Society for Pharmacology and Experimental Therapeutics
View Full Text

MolPharm articles become freely available 12 months after publication, and remain freely available for 5 years. 

Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page. 

 

  • Click here for information on institutional subscriptions.
  • Click here for information on individual ASPET membership.

 

Log in using your username and password

Forgot your user name or password?

Purchase access

You may purchase access to this article. This will require you to create an account if you don't already have one.
PreviousNext
Back to top

In this issue

Molecular Pharmacology: 73 (5)
Molecular Pharmacology
Vol. 73, Issue 5
1 May 2008
  • Table of Contents
  • Table of Contents (PDF)
  • About the Cover
  • Index by author
  • Back Matter (PDF)
  • Editorial Board (PDF)
  • Front Matter (PDF)
Download PDF
Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for sharing this Molecular Pharmacology article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
In Vivo Imaging Reveals Selective Peroxisome Proliferator Activated Receptor Modulator Activity of the Synthetic Ligand 3-(1-(4-Chlorobenzyl)-3-t-butylthio-5-isopropylindol-2-yl)-2,2-dimethylpropanoic acid (MK-886)
(Your Name) has forwarded a page to you from Molecular Pharmacology
(Your Name) thought you would be interested in this article in Molecular Pharmacology.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
Research ArticleArticle

In Vivo Imaging Reveals Selective Peroxisome Proliferator Activated Receptor Modulator Activity of the Synthetic Ligand 3-(1-(4-Chlorobenzyl)-3-t-butylthio-5-isopropylindol-2-yl)-2,2-dimethylpropanoic acid (MK-886)

Andrea Biserni, Fabio Giannessi, Anna Floriana Sciarroni, Ferdinando Maria Milazzo, Adriana Maggi and Paolo Ciana
Molecular Pharmacology May 1, 2008, 73 (5) 1434-1443; DOI: https://doi.org/10.1124/mol.107.042689

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero

Share
Research ArticleArticle

In Vivo Imaging Reveals Selective Peroxisome Proliferator Activated Receptor Modulator Activity of the Synthetic Ligand 3-(1-(4-Chlorobenzyl)-3-t-butylthio-5-isopropylindol-2-yl)-2,2-dimethylpropanoic acid (MK-886)

Andrea Biserni, Fabio Giannessi, Anna Floriana Sciarroni, Ferdinando Maria Milazzo, Adriana Maggi and Paolo Ciana
Molecular Pharmacology May 1, 2008, 73 (5) 1434-1443; DOI: https://doi.org/10.1124/mol.107.042689
Reddit logo Twitter logo Facebook logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
    • Abstract
    • Materials and Methods
    • Results
    • Discussion
    • Acknowledgments
    • Footnotes
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • Cysteine151 in Keap1 Drives CDDO-Me Pharmacodynamic Action
  • Allosteric Modulation of Metabotropic Glutamate Receptor 1
  • Mechanism of Selective Action of Paraherquamide A
Show more Articles

Similar Articles

Advertisement
  • Home
  • Alerts
Facebook   Twitter   LinkedIn   RSS

Navigate

  • Current Issue
  • Fast Forward by date
  • Fast Forward by section
  • Latest Articles
  • Archive
  • Search for Articles
  • Feedback
  • ASPET

More Information

  • About Molecular Pharmacology
  • Editorial Board
  • Instructions to Authors
  • Submit a Manuscript
  • Customized Alerts
  • RSS Feeds
  • Subscriptions
  • Permissions
  • Terms & Conditions of Use

ASPET's Other Journals

  • Drug Metabolism and Disposition
  • Journal of Pharmacology and Experimental Therapeutics
  • Pharmacological Reviews
  • Pharmacology Research & Perspectives
ISSN 1521-0111 (Online)

Copyright © 2023 by the American Society for Pharmacology and Experimental Therapeutics