Structural Development Studies of Subtype-Selective Ligands for Peroxisome Proliferator-Activated Receptors (PPARs) Based on the 3,4-Disubstituted Phenylpropanoic Acid Scaffold as a Versatile Template.

abstract：:Peroxisome proliferator-activated receptor-gamma (PPARgamma), one of three ligand-activated transcription factors named PPAR, has been identified as a molecular target for cancer chemopreventive agents. PPARgamma was initially understood as a regulator of adipocyte differentiation and glucose homeostasis while later o...

journal_title：PPAR research

authors： Sainis I,Vareli K,Karavasilis V,Briasoulis E

更新日期：2008-01-01 00:00:00

abstract：:Peroxisome proliferators activated receptors (PPARs) are ligand-activated nuclear transcription factors that play important roles in lipid and glucose homeostasis. To the extent that PPAR agonists improve diabetic dyslipidaemia and insulin resistance, these agents have been considered to reduce cardiovascular risk. Ho...

journal_title：PPAR research

authors： Calkin AC,Thomas MC

更新日期：2008-01-01 00:00:00

abstract：:INT131 (formerly T0903131, T131, AMG131) is a potent non-thiazolidinedione (TZD) selective peroxisome proliferator-activated receptor gamma modulator (SPPARM) currently in Phase 2 clinical trials for treatment of type-2 diabetes mellitus (T2DM). This new chemical entity represents a second generation SPPARM approach d...

journal_title：PPAR research

authors： Higgins LS,Mantzoros CS

更新日期：2008-01-01 00:00:00

abstract：:Stroke (focal cerebral ischemia) is a leading cause of death and disability among adult population. Many pathological events including inflammation and oxidative stress during the acute period contributes to the secondary neuronal death leading the neurological dysfunction after stroke. Transcriptional regulation of g...

journal_title：PPAR research

authors： Vemuganti R

更新日期：2008-01-01 00:00:00

abstract：:It has been proposed that PPAR-dependent, accelerated catabolism of proinflammatory mediators may contribute to the fast resolution of inflammation. Because retinoid X receptors are obligate heterodimer partners of PPARs, we investigated the impact of deleting hepatocyte-specific RXRalpha on the antiedema effect of PP...

journal_title：PPAR research

authors： Wan YJ,Badr MZ

更新日期：2006-01-01 00:00:00

abstract：:Pancreatic cancer is a devastating disease in which current therapies are inadequate. Separate lines of research have identified the 5-lipoxygenase/leukotriene B(4) receptor pathway and the PPARgamma pathway as potential targets for prevention or treatment of this disease. LY293111 was originally designed as a potent ...

journal_title：PPAR research

authors： Adrian TE,Hennig R,Friess H,Ding X

更新日期：2008-01-01 00:00:00

abstract：:Foxp3(+) regulatory T cells (Tregs) play a critical role in maintaining immune self-tolerance. Reduced number and activity of Tregs are usually found in autoimmune and inflammatory diseases, and enhancing the differentiation of Tregs may be a promising therapeutic strategy. Some reports suggested an anti-inflammatory ...

journal_title：PPAR research

authors： Zhou Z,Liang Y,Gao Y,Kong W,Feng J,Wang X

更新日期：2012-01-01 00:00:00

abstract：:Peroxisome proliferator-activated receptors (PPAR alpha, beta/delta and gamma) play a key role in metabolic regulatory processes and gene regulation of cellular metabolism, particularly in the cardiovascular system. Moreover, PPARs have various extra metabolic roles, in circadian rhythms, inflammation and oxidative st...

journal_title：PPAR research

authors： Lecarpentier Y,Claes V,Hébert JL

更新日期：2010-01-01 00:00:00

abstract：:Hyperhomocysteinemia, a risk factor for vascular disease, is associated with metabolic syndrome. Our study was aimed at exploring the effect of long-term hyperhomocysteinemia with metabolic disturbances on vascular remodeling. We also studied oxidative stress and expression of PPARγ in the coronary arteriole as a poss...

journal_title：PPAR research

authors： Huo Y,Wu X,Ding J,Geng Y,Qiao W,Ge A,Guo C,Lv J,Bao H,Fan W

更新日期：2018-01-15 00:00:00

abstract：:Colorectal cancer is one of the most common cancers in the world. Dietary fat intake is a major risk factor for colorectal cancer. Some nuclear hormone receptors play an important role in regulating nutrient metabolism and energy homeostasis. Among these receptors, special attention has been focused on the role of per...

journal_title：PPAR research

authors： Park JI,Kwak JY

更新日期：2012-01-01 00:00:00

abstract：:PPAR isotypes are involved in the regulation of cell proliferation, death, and differentiation, with different roles and mechanisms depending on the specific isotype and ligand and on the differentiated, undifferentiated, or transformed status of the cell. Differentiation stimuli are integrated by key transcription fa...

journal_title：PPAR research

authors： Cimini A,Cristiano L,Benedetti E,D'Angelo B,Cerù MP

更新日期：2007-01-01 00:00:00

abstract：:The peroxisome proliferator-activated receptors (PPARs), which are ligand-inducible transcription factors expressed in a variety of tissues, have been shown to perform key roles in lipid homeostasis. In physiological situations such as fasting and physical exercise, one PPAR subtype, PPARdelta, triggers a transcriptio...

journal_title：PPAR research

authors： de Lange P,Lombardi A,Silvestri E,Goglia F,Lanni A,Moreno M

更新日期：2008-01-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) is a ligand-activated transcription factor with essential functions in the regulation of lipid catabolism, glucose homeostasis, and inflammation, which makes it a potentially relevant drug target for the treatment of major human diseases. In additi...

journal_title：PPAR research

authors： Müller R,Rieck M,Müller-Brüsselbach S

更新日期：2008-01-01 00:00:00

abstract：:Nitrooleic acid (OA-NO2) is endogenous ligands for peroxisome proliferator-activated receptors. The present study was aimed at investigating the beneficial effects of OA-NO2 on the lipid metabolism and liver steatosis in deoxycorticosterone acetate- (DOCA-) salt induced hypertensive mice model. Male C57BL/6 mice were ...

journal_title：PPAR research

authors： Wang H,Sun J,Jia Z,Yang T,Xu L,Zhao B,Yu K,Wang R

更新日期：2015-01-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor gamma (PPARγ) activation decreased serum testosterone (T) in women with hyperthecosis and/or polycystic ovary syndrome and reduced the conversion of androgens to estradiol (E2) in female rats. This implies modulation of female sex steroid hormones by PPARγ. It is not clear if...

journal_title：PPAR research

authors： Mansour M,Coleman E,Dennis J,Akingbemi B,Schwartz D,Braden T,Judd R,Plaisance E,Stewart LK,Morrison E

更新日期：2009-01-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor-gamma (PPAR-gamma) is a member of the nuclear receptor (NR) superfamily of ligand-activated transcriptional factors. Among other functions, PPAR-gamma acts as a key regulator of the adipogenesis. Since several cytokines (IL-1, TNF-alpha, TGF-beta) had been known to inhibit ad...

journal_title：PPAR research

authors： Takada I,Kouzmenko AP,Kato S

更新日期：2010-01-01 00:00:00

abstract：:The PPAR nuclear receptor family has acquired great relevance in the last decade, which is formed by three different isoforms (PPARα, PPARβ/δ, and PPAR ϒ). Those nuclear receptors are members of the steroid receptor superfamily which take part in essential metabolic and life-sustaining actions. Specifically, PPARG has...

journal_title：PPAR research

authors： Bandera Merchan B,Tinahones FJ,Macías-González M

更新日期：2016-01-01 00:00:00

abstract：:PPARs are ligand-activated transcriptional factors that belong to the nuclear receptor superfamily. Among them, PPAR alpha and PPAR gamma are prone to exert an antiangiogenic effect, whereas PPAR beta/delta has an opposite effect in physiological and pathological conditions. Angiogenesis has been known as a hallmark o...

journal_title：PPAR research

authors： Du S,Wagner N,Wagner KD

更新日期：2020-08-13 00:00:00

abstract：:Pioglitazone (Pio) is a thiazolidinedione (TZD) insulin-sensitizing drug whose effects result predominantly from its modulation of the transcriptional activity of peroxisome proliferator-activated-receptor-gamma (PPARγ). Pio is used to treat human insulin-resistant diabetes and also frequently considered for treatment...

journal_title：PPAR research

authors： Kulkarni S,Huang J,Tycksen E,Cliften PF,Rudnick DA

更新日期：2020-09-10 00:00:00

abstract：:Aster glehni is well known for its therapeutic properties. This study was performed to investigate the effects of A. glehni on nonalcoholic fatty liver disease (NAFLD) in atherosclerotic condition, by determining the levels of biomarkers related to lipid metabolism and inflammation in serum, liver, and adipose tissue....

journal_title：PPAR research

authors： Lee YJ,Jang YN,Han YM,Kim HM,Jeong JM,Son MJ,Jin CB,Kim HJ,Seo HS

更新日期：2017-01-01 00:00:00

abstract：:Infection with Mycobacterium tuberculosis (TB) induces pulmonary immunopathology mediated by classical Th1 type of acquired immunity with hepatic involvement in up to 80% of disseminated cases. Since PPAR agonists cause immune responses characterized by a decrease in the secretion of Th1 cytokines, we investigated the...

journal_title：PPAR research

authors： Badr MZ,Shnyra A,Zoubine M,Norkin M,Herndon B,Quinn T,Miranda RN,Cunningham ML,Molteni A

更新日期：2007-01-01 00:00:00

abstract：:Peroxisome proliferator-activated receptors (PPARs) are ligand-activated transcription factors belonging to the nuclear hormone receptor superfamily. Their discovery in the 1990s provided insights into the cellular mechanisms involved in the control of energy homeostasis, the regulation of cell differentiation, prolif...

journal_title：PPAR research

authors： Han SW,Roman J

更新日期：2008-01-01 00:00:00

abstract：:Protein farnesylation is required for the activation of multiple proteins involved in cell differentiation and function. In white adipose tissue protein, farnesylation has shown to be essential for the successful differentiation of preadipocytes into adipocytes. We hypothesize that protein farnesylation is required fo...

journal_title：PPAR research

authors： Rivas D,Akter R,Duque G

更新日期：2007-01-01 00:00:00

abstract：:The upregulation of peroxisome proliferator-activated receptor gamma (PPARG) has been shown to increase the chemosensitivity of several human cancers. This study is aimed at studying if PPARG sensitizes hypopharyngeal squamous cell carcinoma (HSCC) in chemotherapeutic treatments and at dissecting possible mechanisms o...

journal_title：PPAR research

authors： Lian M,Chen J,Shen X,Hou L,Fang J

更新日期：2020-04-22 00:00:00

abstract：:High mobility group box 1 (HMGB1) is a ubiquitous nuclear DNA-binding protein whose function is dependent on its cellular location. Extracellular HMGB1 is regarded as a delayed mediator of proinflammatory cytokines for initiating and amplifying inflammatory responses, whereas nuclear HMGB1 has been found to prevent ca...

journal_title：PPAR research

authors： Jia Z,Xue R,Liu G,Li L,Yang J,Pi G,Ma S,Kan Q

更新日期：2014-01-01 00:00:00

abstract：:Restricted feeding (RF) during daytime is associated with anticipatory activity before feeding, marked hyperphagia after mealtime, adjustments in hepatic metabolism, and the expression of a food-entrained oscillator (FEO). 24 h rhythmicity of liver PPARα, β, and γ, peroxisomal markers (PMP70, AOX, and catalase), and f...

journal_title：PPAR research

authors： Rivera-Zavala JB,Báez-Ruiz A,Díaz-Muñoz M

更新日期：2011-01-01 00:00:00

abstract：:Background. This study was performed to investigate the influence of a short-term treatment with pioglitazone versus placebo on inflammatory activation of mononuclear cells (mRNA expression/protein secretion of inflammatory markers). Methods and Results. Sixty-three patients with well-controlled type 2 diabetes (52 ma...

journal_title：PPAR research

authors： Pfützner A,Weise A,Pfützner-Riehn E,Lübben G,Morcos M,Karagiannis E,Weber M,Forst T

更新日期：2011-01-01 00:00:00

abstract：:Acute attacks of multiple sclerosis (MS) are most commonly treated with glucocorticoids, which can provide life-saving albeit only temporary symptomatic relief. The mechanism of action (MOA) is now known to involve induction of indoleamine 2,3-dioxygenase (IDO) and interleukin-10 (IL-10), where IL-10 requires subseque...

journal_title：PPAR research

authors： Penberthy WT

更新日期：2009-01-01 00:00:00

abstract：:Cells can shift their metabolism between glycolysis and oxidative phosphorylation to enact their cell fate program in response to external signals. Widely distributed α1-adrenergic receptors (ARs) are physiologically stimulated during exercise, were reported to associate with the activating energetic AMPK pathway, and...

journal_title：PPAR research

authors： Lee YJ,Kim HS,Seo HS,Na JO,Jang YN,Han YM,Kim HM

更新日期：2020-02-01 00:00:00

abstract：:Peroxisome proliferator-activated receptor γ (PPARγ) forms a heterodimeric DNA-binding complex with retinoid X receptors (RXRs). It has been reported that the effect of the PPAR agonist is reduced in hepatocyte RXR-deficient mice. Therefore, it is suggested that the endogenous RXR ligand is involved in the PPARγ agoni...

journal_title：PPAR research

authors： Yamamoto A,Kakuta H,Miyachi H,Sugimoto Y

更新日期：2011-01-01 00:00:00