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Pharmaceuticals
Special Issues
PPARs: Pharmacological Roles of Agonists and Antagonists in Experimental Models
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PPARs: Pharmacological Roles of Agonists and Antagonists in Experimental Models

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: closed (25 January 2021) | Viewed by 6084

Special Issue Editors

Prof. Dr. Luigi Brunetti

E-Mail Website
Guest Editor
Department of Pharmacy, “G. d’Annunzio” University, Via dei Vestini 31, 66100 Chieti, Italy
Interests: emotional behavior; anxiety; depression; inflammation; oxidative stress; obesity
Special Issues, Collections and Topics in MDPI journals
Dr. Sheila Leone

E-Mail Website
Guest Editor
Department of Pharmacy, “G. d’Annunzio” University, Via dei Vestini 31, 66100 Chieti, Italy
Interests: emotional behavior; anxiety; depression; inflammation; oxidative stress; obesity
Special Issues, Collections and Topics in MDPI journals
Dr. Lucia Recinella

E-Mail
Guest Editor
Department of Pharmacy, “G. d’Annunzio” University, Via dei Vestini 31, 66100 Chieti, Italy
Interests: hemotional behavior; anxiety; depression; psychiatric disorder

Special Issue Information

Dear Colleagues,

Peroxisome Proliferator-Activated Receptors (PPARs) are important targets in various diseases, including obesity, metabolic syndrome, diabetes, and nonalcoholic fatty liver disease. PPARs are transcription factors that belong to the nuclear receptor superfamily. There are three subtypes of PPARs, designated as PPARα, γ, and β/δ, which exhibit different tissue expression profiles and modulate specific physiological functions. PPARs play a critical role in regulating the expression of multiple genes involved in the modulation of both glucose and lipid metabolism and energy homeostasis. Recent studies have shown that the activation of PPARs not only regulates multiple metabolic pathways, but also mediates various biological effects related to inflammation, apoptosis, oxidative stress, and vascular function.

The number of molecular drugs binding the PPAR is continuously increasing. The process of drug development consists of multiple steps, including the initial discovery of drugs that can be used as therapeutics; the preclinical and clinical validation of their efficacy and toxicity; and the review, approval, and postmarketing surveillance of drugs by regulatory authorities. In this Special Issue, we invite authors to contribute articles focusing on PPARs and their analogs, with the hopes of increasing the efficiency of the process and identifying drugs that can be used to prevent and/or treat diseases for which effective medications are currently lacking.

Prof. Dr. Luigi Brunetti
Dr. Sheila Leone
Dr. Lucia Recinella
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • PPARs
  • Disease model
  • Drug repositioning

Published Papers (2 papers)

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Research

22 pages, 4394 KiB  
Article
Fenofibrate Protects against Retinal Dysfunction in a Murine Model of Common Carotid Artery Occlusion-Induced Ocular Ischemia
by Deokho Lee, Yohei Tomita, Yukihiro Miwa, Heonuk Jeong, Kiwako Mori, Kazuo Tsubota and Toshihide Kurihara
Pharmaceuticals 2021, 14(3), 223; https://doi.org/10.3390/ph14030223 - 07 Mar 2021
Cited by 11 | Viewed by 3860
Abstract
Ocular ischemia is a common cause of blindness and plays a detrimental role in various diseases such as diabetic retinopathy, occlusion of central retinal arteries, and ocular ischemic syndrome. Abnormalities of neuronal activities in the eye occur under ocular ischemic conditions. Therefore, protecting [...] Read more.
Ocular ischemia is a common cause of blindness and plays a detrimental role in various diseases such as diabetic retinopathy, occlusion of central retinal arteries, and ocular ischemic syndrome. Abnormalities of neuronal activities in the eye occur under ocular ischemic conditions. Therefore, protecting their activities may prevent vision loss. Previously, peroxisome proliferator-activated receptor alpha (PPARα) agonists were suggested as promising drugs in ocular ischemia. However, the potential therapeutic roles of PPARα agonists in ocular ischemia are still unknown. Thus, we attempted to unravel systemic and ocular changes by treatment of fenofibrate, a well-known PPARα agonist, in a new murine model of ocular ischemia. Adult mice were orally administered fenofibrate (60 mg/kg) for 4 days once a day, followed by induction of ocular ischemia by unilateral common carotid artery occlusion (UCCAO). After UCCAO, fenofibrate was continuously supplied to mice once every 2 days during the experiment period. Electroretinography was performed to measure retinal functional changes. Furthermore, samples from the retina, liver, and blood were subjected to qPCR, Western blot, or ELISA analysis. We found that fenofibrate boosted liver function, increased serum levels of fibroblast growth factor 21 (FGF21), one of the neuroprotective molecules in the central nervous system, and protected against UCCAO-induced retinal dysfunction. Our current data suggest a promising fenofibrate therapy in ischemic retinopathies. Full article
(This article belongs to the Special Issue PPARs: Pharmacological Roles of Agonists and Antagonists in Experimental Models)
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10 pages, 2411 KiB  
Article
Effects of Selective Peroxisome Proliferator Activated Receptor Agonists on Corneal Epithelial Wound Healing
by Yutaro Tobita, Takeshi Arima, Yuji Nakano, Masaaki Uchiyama, Akira Shimizu and Hiroshi Takahashi
Pharmaceuticals 2021, 14(2), 88; https://doi.org/10.3390/ph14020088 - 25 Jan 2021
Cited by 7 | Viewed by 1640
Abstract
The effects of each subtype-selective peroxisome proliferator activated receptor (PPAR) agonist (α, β/δ, γ) on corneal epithelial wound healing were investigated using a rat corneal alkali burn model. After the alkali burn, each PPAR agonist or vehicle ophthalmic solution was instilled topically onto [...] Read more.
The effects of each subtype-selective peroxisome proliferator activated receptor (PPAR) agonist (α, β/δ, γ) on corneal epithelial wound healing were investigated using a rat corneal alkali burn model. After the alkali burn, each PPAR agonist or vehicle ophthalmic solution was instilled topically onto the rat’s cornea. Corneal epithelial healing processes were evaluated by fluorescein staining. Pathological analyses and real-time reverse transcription polymerase chain reactions were performed to evaluate Ki67 (proliferative maker) expression and inflammatory findings. The area of the corneal epithelial defect at 12 h and 24 h after the alkali burn was significantly smaller in each PPAR group than in the vehicle group. Ki67 mRNA expression was increased in the PPARβ/δ group, whereas mRNA expressions of inflammatory cytokines were suppressed in all of the PPAR agonist groups. Nuclear factor kappa B (NF-κB) was the most suppressed in the PPARγ group. The accelerated corneal epithelial healing effects of each PPAR ligand were thought to be related to the promotion of proliferative capacity and inhibition of inflammation. Full article
(This article belongs to the Special Issue PPARs: Pharmacological Roles of Agonists and Antagonists in Experimental Models)
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