Peroxisome ppar. Medical search. Frequent questions

Mono(2-ethylhexyl) tetrabromophthalate, halogenated bisphenols and phenols, and hydroxylated PBDEs were found to be potent PPARγ ligands. (duke.edu)
A 3-16% increase in PPARγ binding potency was observed following bioactivation of the dust using rat hepatic S9 fractions.Our results suggest that several flame retardants are potential PPARγ ligands and that metabolism may lead to increased binding affinity. (duke.edu)
There are several suggested hypotheses for the poor translation from animal to human research evidence such as the potency and selectivity of PPAR ligands, sex-related variability, and species differences in the distribution and signaling of PPAR. (wikipedia.org)
L'effet de ligands de PPAR et de ROR[alpha] sur certains paramètres de l'inflammation induits par le LPS ou l'IL-1[bêta] a ensuite été étudié. (univ-lorraine.fr)
When coadministered, a significant synergistic effect of PPARγ and RXR ligands was observed. (hal.science)
In combination, these data demonstrate that activation of the RXR/PPARγ heterodimer protects against colon inflammation and suggest that combination therapy with both RXR and PPARγ ligands might hold promise in the clinic due to their synergistic effects. (hal.science)
Here we report that antidiabetic thiazolidinediones (TZDs) and other ligands for the nuclear receptor PPARγ dramatically upregulate oxidized LDL receptor 1 (OLR1) in adipocytes by facilitating the exchange of coactivators for corepressors on the OLR1 gene in cultured mouse adipocytes. (jci.org)
While the physiological role of adipose tissue in cholesterol and oxLDL metabolism remains to be established, the induction of OLR1 is a potential means by which PPARγ ligands regulate lipid metabolism and insulin sensitivity in adipocytes. (jci.org)
With the involvement of PPARs in many diverse metabolic pathways there is great clinical interest in the potential utility of PPAR ligands for the treatment of cancer, inflammation, psoriasis, atherosclerosis, dyslipidaemia, neurological disorders, obesity and diabetes. (sigmaaldrich.com)
A potential modifier of this response could be through receptor activation (peroxisome proliferator-activated receptor - PPAR), as PFOA and PFOS are known PPAR ligands and modulate inflammatory immune pathways. (cdc.gov)

The transcriptional coactivator peroxisome proliferator activated receptor (PPAR)gamma coactivator-1 alpha and the nuclear receptor PPAR alpha control the expression of glycerol kinase and metabolism genes independently of PPAR gamma activation in human white adipocytes. (unil.ch)
PPAR-alpha and PPAR-gamma are the molecular targets of a number of marketed drugs. (wikipedia.org)
PPARγ (gamma) is the main target of the drug class of thiazolidinediones (TZDs), used in diabetes mellitus and other diseases that feature insulin resistance. (wikipedia.org)
Introduction: The multifunctional nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-γ) has potent anti-fibrotic effects, and its expression and activity are impaired in patients with systemic sclerosis (SSc). (northwestern.edu)
Enfin, les mécanismes d'action de la I5d-PGJ2, ligand physiologique de PPAR[gamma], et les cibles intracellulaires éventuelles dans les voies transcriptionnelles, NF-[kappa]B et AP-1, ont été explorés. (univ-lorraine.fr)
Le peu d'effet observé avec la troglitazone suggère que l'action de la 15d-PGJ2 dans les chondrocytes et les synoviocytes est principalement indépendante de PPAR[gamma]. (univ-lorraine.fr)
ZNF746) was initially identified as a novel co-substrate of parkin and PINK1 that leads to Parkinson's disease (PD) by disrupting mitochondrial biogenesis through peroxisome proliferator-activated receptor gamma (PPARγ) coactivator -1α (PGC-1α) suppression. (nature.com)
Originally discovered as a chief regulatory protein of glucose and lipid metabolism and cell differentiation, the peroxisome proliferator-activated receptor gamma (PPARγ) is a ligand-activated transcription factor of the nuclear hormone receptor superfamily 8 . (nature.com)
Methods: Peroxisome Proliferator-Activated Receptor gamma (PPARγ) ligand binding assays were used to identify obesogens. (nist.gov)
Pioglitazone is a potent agonist for peroxisome proliferator-activated receptor-gamma (PPARγ). (globalrph.com)
T3D-959, an oral dual delta/gamma peroxisome proliferator-activated nuclear receptor (PPAR) agonist, has shown promise in a phase 2 randomized, placebo-controlled study of adults with mild-to-moderate Alzheimer's disease (AD). (medscape.com)
Uniquely, this drug also activates PPAR gamma, which may provide potential additive or synergistic effects in regulating dysfunctional brain glucose energy and lipid metabolism in AD. (medscape.com)

A fourth class of dual PPAR agonists, so-called glitazars, which bind to both the α and γ PPAR isoforms, are currently under active investigation for treatment of a larger subset of the symptoms of the metabolic syndrome. (wikipedia.org)
In addition, there is continuing research and development of new dual α/δ and γ/δ PPAR agonists for additional therapeutic indications, as well as "pan" agonists acting on all three isoforms. (wikipedia.org)
Isoflavones genistein and daidzein bind to and transactivate all three PPAR isoforms, α, δ, and γ. (wikipedia.org)
Peroxisome proliferator activated-receptor (PPAR) isoforms, α and γ, function as important coregulators of energy (lipid) homeostasis. (northwestern.edu)
Of the two PPARγ isoforms, PPARγ1 and PPARγ2 generated by alternative splicing, PPARγ1 isoform is expressed in liver and other tissues, whereas PPARγ2 isoform is expressed exclusively in adipose tissue where it regulates adipogenesis and lipogenesis. (northwestern.edu)
There are two PPARγ isoforms, PPARγ1 and γ2. (biomedcentral.com)
X-ray crystallography of human PPAR isoforms has revealed important residues responsible for ligand binding, heterodimerisation and co-factor interactions. (sigmaaldrich.com)

PPAR agonists are drugs which act upon the peroxisome proliferator-activated receptor. (wikipedia.org)
The main classes of PPAR agonists are: An endogenous compound, 7(S)-Hydroxydocosahexaenoic Acid (7(S)-HDHA), which is a Docosanoid derivative of the omega-3 fatty acid DHA was isolated as an endogenous high affinity ligand for PPAR-alpha in the rat and mouse brain. (wikipedia.org)
PPAR dual agonists: are they opening Pandora's Box? (wikipedia.org)
A role for the RXR/PPARγ heterodimer in the protection against colon inflammation was explored by the use of selective RXR and PPARγ agonists. (hal.science)
TNBS-induced colitis was significantly reduced by the administration of both PPARγ and RXR agonists. (hal.science)
In fact, PPAR agonists - which help activate PPARs - are one class of new diabetes drugs. (stumptuous.com)
PPARα agonists (fibrates) have shown therapeutic utility as lipid lowering agents whereas PPARγ agonists such as the glitazones (thiazolidinediones) are marketed as antidiabetic agents. (sigmaaldrich.com)
The rationale for evaluating PPAR agonists in AD is based on the hypothesis that sporadic AD is fundamentally an age-related metabolic disease. (medscape.com)

PPARα regulates fatty acid oxidation primarily in liver and to a lesser extent in adipose tissue, whereas PPARγ serves as a key regulator of adipocyte differentiation and lipid storage. (northwestern.edu)
These results suggest that a high level of PPARγ in mouse liver is sufficient for the induction of adipogenic transformation of hepatocytes with adipose tissue-specific gene expression and lipid accumulation. (northwestern.edu)
OLR1 expression in white adipose tissue is increased in obesity and is further induced by PPARγ ligand treatment in vivo. (jci.org)
PPARγ is highly expressed in adipose tissue and is a key transcription factor involved in the terminal differentiation of white and brown adipose tissue. (sigmaaldrich.com)
PPARα and LXRα were mainly expressed in liver, while PPARγ1 predominated in adipose tissue and large intestine. (diabetesjournals.org)
We found that PPARγ2 mRNA was a minor isoform, even in adipose tissue, thus causing question of its role in humans. (diabetesjournals.org)
PPAR receptors are found in tissues important for insulin action such as adipose tissue, skeletal muscle, and liver. (globalrph.com)

Ligand binding activity of indoor dust and its bioactivated extracts were also investigated.We used a commercially available fluorescence polarization ligand binding assay to investigate the binding potency of flame retardants and dust extracts to human PPARγ ligand-binding domain. (duke.edu)
SB1495 occupies the Arm3 region near the Ω loop of the PPARγ ligand-binding domain, whereas its enantiomeric analogue SB1494 binds to the Arm2 region. (rcsb.org)

The increase in liver weights was due to activation of PPARα and peroxisome proliferation. (elifesciences.org)
Interestingly, PPARα and β expression is reactivated in the adult epidermis after various stimuli, resulting in keratinocyte proliferation and differentiation such as tetradecanoylphorbol acetate topical application, hair plucking, or skin wound healing. (hal.science)
PPARα is mainly involved in the early inflammation phase of the healing, whereas PPARβ is implicated in the control of keratinocyte proliferation. (hal.science)
No evidence of peroxisome proliferation in the liver was reported. (canada.ca)
In liver, PPARα regulates lipid metabolism and in rodents, but not in man, PPARα activation induces hepatomegaly and proliferation of liver peroxisomes. (sigmaaldrich.com)

RNA-sequence analysis revealed that curcumin intake affected hepatic lipid metabolism via the peroxisome proliferator-activated receptor (PPAR) pathway, especially PPARα activation, resulting in increased Apoa2 mRNA expression. (elifesciences.org)
Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors and commonly play an important role in the regulation of lipid homeostasis. (biomedcentral.com)
DNA microarray analyses using these cell lines were performed with or without adding each subtype ligand and provided much important information on the PPAR target genes involved in lipid metabolism, transport, storage and other activities. (biomedcentral.com)
Members of the peroxisome proliferator-activated receptor (PPAR) family might be involved in pathologies with altered lipid metabolism. (diabetesjournals.org)
Activation of PPARγ nuclear receptors modulates the transcription of a number of insulin responsive genes involved in the control of glucose and lipid metabolism. (globalrph.com)

PPARα is expressed in the liver, kidney, heart and muscle where it regulates energy homeostasis. (biomedcentral.com)
Activation of PPARγ nuclear receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. (globalrph.com)

PPARδ is ubiquitously expressed in tissues and has been implicated in energy metabolism in both adipose and skeletal muscle. (sigmaaldrich.com)
In addition, PPARγ mRNA was barely detectable in skeletal muscle, suggesting that improvement of insulin resistance with thiazolidinediones may not result from a direct effect of these agents on PPARγ in muscle. (diabetesjournals.org)

Northern blotting and gene expression profiling results showed that adipocyte-specific genes and lipogenesis-related genes are highly induced in PPARα -/- livers with PPARγ1 over-expression. (northwestern.edu)
Of interest is that hepatic steatosis per se, induced either by feeding a diet deficient in choline or developing in fasted PPARα -/- mice, failed to induce the expression of these PPARγ-regulated adipogenesis-related genes in steatotic liver. (northwestern.edu)
To identify human PPARs-responsive genes, we established tetracycline-regulated human hepatoblastoma cell lines that can be induced to express each human PPAR and investigated the gene expression profiles of these cells. (biomedcentral.com)
Interestingly, it was noted that while ligand-activated PPARδ induced target gene expression, unliganded PPARδ repressed these genes. (biomedcentral.com)
Moreover, we identified that PARIS actively modulates expression of PPARγ target genes by physically binding to the promoter regions. (nature.com)
In addition, PPARγ-responsive genes also participate in the regulation of fatty acid metabolism. (globalrph.com)

Les récepteurs nucléaires PPAR ("peroxisome proliferator-activated receptor")et ROR[alpha] (" retinoic acid receptor-related orphan receptor alpha") sont des facteurs de transcription impliqués notamment dans la différenciation adipocytaire, le métabolisme lipidique et l'homéostasie du glucose. (univ-lorraine.fr)

Peroxisome proliferator activated receptors (PPARs) are members of the nuclear hormone receptor superfamily of ligand-activated transcription factors that are related to retinoid, steroid and thyroid hormone receptors. (sigmaaldrich.com)
Coactivator proteins such as SRC1 and CBP/p300 are recruited by agonist bound receptors and promote initiation of transcription by remodelling the chromatin structure while coactivators such as the PPAR binding protein (PBP) and TRAP220 interact directly with the transcriptional machinery. (sigmaaldrich.com)

Many of these contaminants act via the activation of the peroxisome proliferator-activated receptor γ (PPARγ) nuclear receptor.Our goal was to determine the PPARγ ligand binding potency of several major flame retardants, including polybrominated diphenyl ethers (PBDEs), halogenated phenols and bisphenols, and their metabolites. (duke.edu)

Peroxisome proliferator-activated receptor (PPAR)- modulates substrate metabolism and inflammatory responses. (tam-receptor.com)

Multivariate evaluation indicated that existence of the D-(+)-Xylose -tocopherol, however, not a thiazolidinedione, moiety in the check compound was considerably related to better contractile function and lactate uptake and lower cytokine appearance during I/R. We conclude that PPAR- activation isn't protective within a porcine style of myocardial I/R. Defensive ramifications of troglitazone are due to its D-(+)-Xylose -tocopherol moiety. (tam-receptor.com)
These results, together with prior rat research, suggest interspecies distinctions in the response to PPAR- activation in the center. (tam-receptor.com)
The 7(S) enantiomer bound with micromolar affity to PPAR alpha with 10 fold higher affinity compared to the (R) enantiomer and could trigger dendritic activation.PPARα (alpha) is the main target of fibrate drugs, a class of amphipathic carboxylic acids (clofibrate, gemfibrozil, ciprofibrate, bezafibrate, and fenofibrate). (wikipedia.org)
A relatively recent avenue of drug research in treating depression and drug addiction is through PPARα and PPARγ activation. (wikipedia.org)
All fractions showed bioactivity in PPAR activation assays, but quantitative responses showed marked fruit-to-fruit variability, highlighting the need to bulk fruit prior to extraction for activity-guided fractionation of bioactive components. (qld.gov.au)
The peroxisome proliferator-activated receptor γ (PPARγ) is highly expressed in the colon mucosa and its activation has been reported to protect against colitis. (hal.science)
Consistent with this relatively high divergence among the subtype-specific ligand binding domains, differential activation of PPARs by endogenous and exogenous compounds may account for the specific biological activity of the three PPAR subtypes [ 2 , 3 ]. (biomedcentral.com)
To achieve this versatility PPARγ interacts with a range of additional molecules required for both transcriptional co-activation and structural changes that promote its dimerization for DNA binding. (nature.com)

Adenovirus-PPARγ1 injected into the tail vein induced hepatic steatosis in PPARα -/- mice. (northwestern.edu)
We conclude that excess PPARγ activity can lead to the development of a novel type of adipogenic hepatic steatosis. (northwestern.edu)

It has been shown that agonism of PPARδ changes the body's fuel preference from glucose to lipids. (wikipedia.org)
Our results may contribute to the development of a new generation of antidiabetic drugs that selectively block PPARγ phosphorylation without classical agonism. (rcsb.org)

DOSS was found to be a significant obesogen by ligand binding assays, PPAR-driven luciferase induction in vivo and fat cell induction. (nist.gov)
In addition, thiazolidinediones improve insulin resistance in vivo by activating PPARγ. (diabetesjournals.org)

Using PPARα, β, and γ mutant mice, we demonstrate that PPARα and β are important for the rapid epithelialization of a skin wound and that each of them plays a specific role in this process. (hal.science)
PPARγ1/− and RXRα1/− mice both displayed a significantly enhanced susceptibility to 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis compared with their wild-type littermates. (hal.science)

PPARα is expressed in tissues exhibiting high rates of β-oxidation such as liver, kidney, heart and muscle. (sigmaaldrich.com)
PPARδ is abundant in many tissues during development especially in the adult rat digestive tract where a high rate of cell renewal and differentiation is required. (sigmaaldrich.com)
PPARβ mRNA was present in all the tissues tested at low levels. (diabetesjournals.org)

When PPAR-ƴs are going gangbusters, inflammation goes down. (stumptuous.com)

Rosiglitazone was used as a positive control.Most of the tested compounds exhibited dose-dependent binding to PPARγ. (duke.edu)

Indeed, some of these PPARγ activators have already been suggested as potential targets for the treatment of several neurodegenerative disorders including PD, Alzheimer's disease, Huntington's disease and amyotrophic lateral sclerosis (ALS) 13 . (nature.com)

b) L-165041 has 2.6-fold selectivity for murine PPARδ/PPARγ but is 10-fold selective for human PPARδ/PPARγ and PPARα. (sigmaaldrich.com)
c) Human PPARδ/PPARα 2.5 fold selectivity and murine PPARδ/PPARγ selectivity 2-fold. (sigmaaldrich.com)

Results DIM, but not I3C, increased adipocyte differentiation through upregulation of peroxisome proliferator‐activated receptor γ and CCAAT/enhancer‐binding protein α. (researchgate.net)

The PPARγ binding activity of house dust extracts at levels comparable to human exposure warrants further studies into agonistic or antagonistic activities and their potential health effects. (duke.edu)

We studied the involvement of PPARγ and its heterodimeric partner, the retinoid X receptor (RXR) in intestinal inflammatory responses. (hal.science)
There is evidence that both PPARα and PPARγ could interfere with atherogenesis, in part by exerting an anti-inflammatory activity. (sigmaaldrich.com)
Expose human cell lines to PFOA and PFOS at a range of doses of human-relevance and identify significant alterations in pro-inflammatory gene expression (IL-1B, NF-kB, MyD88), including the role of PPAR in modulating the immune response. (cdc.gov)

PPARα activates fatty acid catabolism, stimulates gluconeogenesis and ketone body synthesis and is involved in the control of lipoprotein assembly [ 4 ]. (biomedcentral.com)

ITT, GTT, and MTT showed that CS rats were neither insulin resistant nor glucose intolerant, but mRNA expression of cholecystokinin (CCK) in the duodenum was higher and that of CPT1, PPARα, and PGC1α in liver were lower than in CR rats. (frontiersin.org)
Using a rational drug discovery approach, we recently developed SB1495, a novel reversible covalent inhibitor of the cyclin-dependent kinase 5 (Cdk5)-mediated phosphorylation of PPARγ at Ser245, a key factor in the insulin-sensitizing effect of PPARγ-targeted drugs. (rcsb.org)

Three subtypes, PPARα, PPARβ/δ and PPARγ, have been identified and these subtypes with a high degree of sequence conservation of each subtype across various species, have been characterized. (biomedcentral.com)

PPARγ3 is a splicing variant of PPARγ1 and gives rise to the same protein. (biomedcentral.com)

Taken together, these results demonstrate that curcumin is a PPARα activator and may affect expression levels of proteins involved in amyloid deposition to influence amyloidosis and metabolism in a complex manner. (elifesciences.org)
The expression of each introduced PPAR gene was investigated using the various concentrations of doxycycline in the culture media. (biomedcentral.com)
We found that the expression of each PPAR subtype was tightly controlled by the concentration of doxycycline in these established cell lines. (biomedcentral.com)

We investigated PPAR-γ gene (PPARG) single nucleotide polymorphisms (SNPs) associated with SSc. (northwestern.edu)
Conclusions: A PPARG variant is associated with susceptibility to SSc, consistent with a role of PPAR-γ in the pathogenesis of SSc. (northwestern.edu)

These data identify OLR1 as a novel PPARγ target gene in adipocytes. (jci.org)

The PPAR family of proteins helps regulate blood sugar and triglyceride levels. (medscape.com)

Peroxisome proliferator-activated receptor γ (PPARγ) is a major therapeutic target for the treatment of type 2 diabetes. (rcsb.org)

In addition and very interestingly, PPARβ mutant primary keratinocytes show impaired adhesion and migration properties. (hal.science)

Scholars@Duke publication: Characterizing the peroxisome proliferator-activated receptor (PPARγ) ligand binding potential of several major flame retardants, their metabolites, and chemical mixtures in house dust. (duke.edu)

T3D-959 is the first PPAR delta-activating compound to be developed for the treatment of AD. (medscape.com)

The results demonstrated that PPARγ functions as a master regulator of PARIS-induced molecular changes at the transcriptome level, confirming that PARIS acts primarily on PGC-1α to lead to neurodegeneration in PD. (nature.com)

Thus, the findings presented here reveal unpredicted roles for PPARα and β in adult mouse epidermal repair. (hal.science)

Anatomy27

Organisms14

Diseases16

Chemicals and Drugs136

Analytical, Diagnostic and Therapeutic Techniques and Equipment20

Psychiatry and Psychology1

Phenomena and Processes47

Disciplines and Occupations1

Technology, Industry, Agriculture1

Information Science3

Ligands10

Gamma12

Isoforms7

Agonists8

Adipose tissue7

Ligand-bindin2

Proliferation5

Lipid5

Regulates2

Skeletal muscle2

Genes6

Receptor alpha1

Receptors2

Nuclear1

Modulates1

Activation8

Hepatic2

Agonism2

Vivo2

Mice2

Tissues3

Inflammation1

Rosiglitazone1

Activators1

Selectivity2

Differentiation1

Dust extracts1

Inflammatory3

Activates1

Insulin2

Subtypes1

Protein1

Expression3

PPARG2

Target gene1

Regulate1

Therapeutic1

Interestingly1

Characterizing1

Compound1

Regulator1

Roles1