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Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression.

Author: HashimotoYuichi, IshikawaMinoru, MakishimaMakoto, NomuraSayaka, ToyotaYosuke

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Overview

This study investigated the structure-activity relationships (SARs) of PPARγ agonist rosiglitazone, focusing on transrepression activity. The authors identified several alkenic analogs of rosiglitazone with more potent transrepression activity and reduced agonistic efficacy, suggesting that selective PPARγ ligands with transrepression-selective activity could be developed for the treatment of inflammatory conditions with reduced side effects.
Paper Details　
Original Abstract of the Article :
Anti-inflammatory effects of peroxisome proliferator-activated receptor gamma (PPRAγ) ligands are thought to be largely due to PPARγ-mediated transrepression. Thus, transrepression-selective PPARγ ligands without agonistic activity or with only partial agonistic activity should exhibi...See full text at original site
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引用元：
https://doi.org/10.1016/j.bmcl.2017.04.061

データ提供：米国国立医学図書館（NLM）

Structure-Activity Relationships of Rosiglitazone for Peroxisome Proliferator-Activated Receptor Gamma Transrepression

This research explores the structure-activity relationships (SARs) of rosiglitazone, a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, focusing on its transrepression activity. The researchers investigated the anti-inflammatory properties of rosiglitazone, aiming to develop PPARγ ligands with enhanced selectivity for transrepression over transactivation. Their findings provide valuable insights into the design of novel PPARγ ligands with potentially improved therapeutic profiles.

Designing PPARγ Ligands with Enhanced Selectivity

The study found that certain modifications to rosiglitazone's structure could enhance its transrepression activity while reducing its agonistic efficacy. These modifications involved altering the alkyl group on the nitrogen atom and exploring the use of alkenic analogs. The researchers identified a compound, 3l, that exhibited significantly stronger transrepressional activity than rosiglitazone or pioglitazone, suggesting a potential advantage in terms of therapeutic efficacy and side effect profile.

Harnessing the Power of Transrepression for Therapeutic Benefit

This research underscores the potential of transrepression-selective PPARγ ligands for treating inflammatory diseases. The researchers' findings highlight the need for continued research into the development of these novel therapeutic agents, paving the way for new treatments with potentially improved efficacy and safety profiles.

Dr. Camel's Conclusion

This research reminds us that even in the vast desert of pharmaceutical research, there are oases of hope. By carefully dissecting the structure-activity relationships of molecules like rosiglitazone, we can unlock new therapeutic possibilities, paving the way for treatments with enhanced efficacy and reduced side effects.

Date :
  1. Date Completed 2017-07-18
  2. Date Revised 2018-12-02
Further Info :

Pubmed ID

28465099

DOI: Digital Object Identifier

10.1016/j.bmcl.2017.04.061

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in preparation
Languages

English

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