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Screening for PPAR Non-Agonist Ligands Followed by Characterization of a Hit, AM-879, with Additional No-Adipogenic and cdk5-Mediated Phosphorylation Inhibition Properties.

Author: BajgelmanMarcio Chaim, Bernardi VideiraNatália, BridiAline Villanova, FigueiraAna Carolina Migliorini, Helena BatistaFernanda Aparecida, Le MaireAlbane, Ribeiro FilhoHelder Veras, TittanegroThais Helena, de Carvalho PereiraJosé Geraldo, de OliveiraPaulo Sérgio Lopes

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

Overview

This study identified a novel non-agonist PPARγ ligand, AM-879, that binds to the receptor without activating it. Unlike traditional PPARγ agonists, AM-879 does not induce adipocyte differentiation or alter gene expression associated with adipogenesis. It inhibits CDK5-mediated phosphorylation of PPARγ, suggesting a potential mechanism for its antidiabetic effects.
Paper Details　
Original Abstract of the Article :
Peroxisome proliferator-activated receptor gamma (PPARγ) is a member of a nuclear receptor superfamily and acts as a ligand-dependent transcription factor, playing key roles in maintenance of adipose tissue and in regulation of glucose and lipid homeostasis. This receptor is the target of thiaz...See full text at original site
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引用元：
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5799700/

データ提供：米国国立医学図書館（NLM）

Screening for PPAR Non-Agonist Ligands: Discovering AM-879

Peroxisome proliferator-activated receptor gamma (PPARγ) plays a crucial role in regulating glucose and lipid homeostasis, making it a target for antidiabetic drugs. However, existing drugs like rosiglitazone and pioglitazone, while effective, come with side effects. This study aims to identify novel PPARγ ligands that do not possess agonist properties, focusing on potential non-agonist ligands that may offer antidiabetic benefits without the associated side effects. The authors describe their screening process, highlighting the discovery of AM-879, a promising non-agonist ligand with potential therapeutic applications in diabetes management.

Beyond Agonism: Seeking New Strategies for Diabetes Treatment

This research challenges traditional approaches to diabetes treatment by exploring the potential of non-agonist PPARγ ligands. By investigating the mechanism of action of AM-879, the authors demonstrate that this non-agonist ligand can interact with PPARγ without triggering full activation, potentially offering a safer and more effective approach to managing diabetes. These findings highlight the need for continued research into alternative strategies for addressing this growing health concern.

New Horizons in Diabetes Management: The Potential of AM-879

This study opens new avenues for developing safer and more effective treatments for diabetes. The discovery of AM-879, a non-agonist PPARγ ligand, provides a promising starting point for exploring alternative therapeutic strategies that minimize side effects while maximizing efficacy. Further research is needed to fully understand the potential of AM-879 and its role in managing diabetes.

Dr. Camel's Conclusion

Imagine a desert oasis where a new spring emerges, offering a refreshing alternative to existing water sources. This research explores the potential of non-agonist PPARγ ligands, representing a promising new avenue for treating diabetes. The discovery of AM-879, a non-agonist ligand with antidiabetic properties, offers hope for a safer and more effective approach to managing this complex disease.
Date :
  1. Date Completed n.d.
  2. Date Revised 2023-11-12
Further Info :

Pubmed ID

29449830

DOI: Digital Object Identifier

PMC5799700

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Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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