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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The challenges of PPARδ selectivity and the medicinal chemistry of most active agonists discovered by different pharmaceutical companies and institutes are focused on.
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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.
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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
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An overview of the various molecular structures that are able to block each of the PPAR subtypes, with a focus on promising therapeutic applications.
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