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Promising role of peroxisome proliferator-activated receptors in respiratory disorders, a review.
Drug Metab Rev
December 2024
Applied Biomedical Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.
Several studies indicate various pharmacological and therapeutic effects of peroxisome proliferator-activated receptors (PPARs) in different disorders. The current review describes the influences of PPARs on respiratory, allergic, and immunologic diseases. Various databases, including PubMed, Science Direct, and Scopus, were searched regarding the effect of PPARs on respiratory and allergic disorders from 1990 to 2024.
View Article and Find Full Text PDFKetamine impairs the performance of male mice in novel recognition object test and reduces the immunoreactivity of GAD in the hippocampus: Role of pioglitazone.
Pharmacol Biochem Behav
December 2024
Programa de Pós-Graduação em Farmacologia, Universidade Federal de Santa Maria, RS, Brazil. Electronic address:
Schizophrenia is a mental disorder characterized by positive, negative, and cognitive symptoms which is treated with antipsychotics. However, these drugs present several side effects and, some schizophrenia symptoms, like cognitive, are difficult to treat. The peroxisome proliferator-activated receptors-gamma (PPAR-γ) are expressed in dopaminergic neurons of the midbrain participating in the modulation of neurotransmitters release like dopamine.
View Article and Find Full Text PDFRole of peroxisome proliferator-activated receptors α and γ in mediating the beneficial effects of β-caryophyllene in a rat model of fragile X syndrome.
Prog Neuropsychopharmacol Biol Psychiatry
December 2024
Dept. Science, Roma Tre University, Rome, Italy; Neuroendocrinology, Metabolism and Neuropharmacology Unit, IRCCS Fondazione Santa Lucia, Rome, Italy. Electronic address:
β-Caryophyllene (BCP) is a naturally occurring sesquiterpene found in numerous plant species, including Cannabis sativa. BCP has shown a high safety profile and a wide range of biological functions, including beneficial effects in neurodegenerative and inflammatory diseases. Here, we used behavioral, pharmacological, and in-silico docking analyses to investigate the effects and mechanism of action of BCP in Fragile X Syndrome (FXS), the most common inherited cause of Autism Spectrum Disorder (ASD) and intellectual disability.
View Article and Find Full Text PDFThe polycomb protein complex interacts with GATA-6/PPARα to inhibit α-MHC expression.
Dev Growth Differ
December 2024
Department of Biochemistry & Molecular Biology, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, China.
Transcription factors collaborate with epigenetic regulatory factors to orchestrate cardiac differentiation for heart development, but the underlying mechanism is not fully understood. Here, we report that GATA-6 induces cardiac differentiation but peroxisome proliferator-activated receptor α (PPARα) reverses GATA-6-induced cardiac differentiation, possibly because GATA-6/PPARα recruits the polycomb protein complex containing EZH2/Ring1b/BMI1 to the promoter of the cardiac-specific α-myosin heavy chain (α-MHC) gene and suppresses α-MHC expression, which ultimately inhibits cardiac differentiation. Furthermore, Ring1b ubiquitylates PPARα and GATA-6.
View Article and Find Full Text PDF-Tosyl Hydrazone Benzopyran, a New Ligand of PPARα Obtained from Mapping the Conformational Space of Its Active Site.
J Chem Inf Model
December 2024
Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis, Instituto Multidisciplinario de Investigaciones Biológicas (IMIBIO-SL). CONICET, Ejército de los Andes 950, 5700 San Luis, Argentina.
We report here a new ligand for the peroxisome-proliferator-activated receptor type α (PPARα), an N-tosyl hydrazone benzopyran that was designed throughout the mapping of the polar zone of the binding site of PPARα; such a compound displays a strong activity on this receptor that is comparable to that of the reference compound WY-14643. For the design of the -tosyl hydrazone benzopyran, we have carried out an exhaustive conformational study of WY-14643 and a previously reported hydrazine benzopyran derivative using conformational potential energy surfaces (PES). This study allowed us to map in a systematic way the entire binding site of the PPARα.
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