PPAR-β/δ agonists for Type 2 diabetes and dyslipidemia: an adopted orphan still looking for a home

@article{Billin2008PPARAF,
  title={PPAR-$\beta$/$\delta$ agonists for Type 2 diabetes and dyslipidemia: an adopted orphan still looking for a home},
  author={Andrew N Billin},
  journal={Expert Opinion on Investigational Drugs},
  year={2008},
  volume={17},
  pages={1465 - 1471}
}
  • A. Billin
  • Published 22 September 2008
  • Medicine, Biology
  • Expert Opinion on Investigational Drugs
Background: The identification of small molecule agonists for the nuclear receptor peroxisome proliferator-activated receptor beta/delta (PPAR-β/δ, NR1C2) has enabled the characterization of this receptor's functions in preclinical models. Subsequently, a number of small molecule agonists of PPAR-β/δ have been progressed into clinical trials. Objective: This review will examine the major preclinical findings that underpin the hypothesis that PPAR-β/δ agonists may be beneficial in treating… 
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Peroxisome Proliferator-Activated Receptor δ: A Target with a Broad Therapeutic Potential for Drug Discovery
TLDR
The identification of small molecule agonists for PPAR-δ has shed some light on the function of this ubiquitously expressed receptor in preclinical models and early clinical studies, and revealed the multiple benefits of PP AR delta (δ) activation on lipid disorders, diabetes, and inflammation.
Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
Targeting Peroxisome Proliferator-activated Receptor delta (PPARδ): A Medicinal Chemistry Perspective.
TLDR
The challenges of PPARδ selectivity and the medicinal chemistry of most active agonists discovered by different pharmaceutical companies and institutes are focused on.
The Opportunities and Challenges of Peroxisome Proliferator-Activated Receptors Ligands in Clinical Drug Discovery and Development
TLDR
84 types of PPAR synthetic ligands introduced to date for the treatment of metabolic and other diseases are summarized and a comprehensive analysis of the current applications and problems of these ligands in clinical drug discovery and development is provided.
Unraveling the Effects of PPARβ/δ on Insulin Resistance and Cardiovascular Disease
PPARβ/δ: A Key Therapeutic Target in Metabolic Disorders
TLDR
The potential of the pharmacological activation of PPARβ/δ as a treatment for human metabolic disorders, including obesity, dyslipidaemia, type 2 diabetes mellitus and non-alcoholic fatty liver disease is described.
Biology and therapeutic applications of peroxisome proliferator- activated receptors.
TLDR
The current and potential medical implications of PPAR ligands in various pathologies, ranging from metabolic disorders to cardiovascular disease, chronic inflammation, neurodegenerative disorders and cancer, are discussed.
A Novel Strategy for Designing the Selective PPAR Agonist by the “Sum of Activity” Model
TLDR
‘sum of activity’ model was employed to design multi-target agonists that fit both α and δ but not γ to avoid side effect and it was proposed that distinct features shown in models (a), (b), (d) but not (c) and (e) should be accounted in designing weight-controlling drugs.
Blocking the Peroxisome Proliferator‐Activated Receptor (PPAR): An Overview
TLDR
An overview of the various molecular structures that are able to block each of the PPAR subtypes, with a focus on promising therapeutic applications.
Modulation of gastrointestinal inflammation and colorectal tumorigenesis by peroxisome proliferator-activated receptor-β/δ (PPARβ/δ).
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