Abstract:
:Fibrates and WY-14643 are widely used as lipid-lowering drugs via modulation of peroxisome proliferator-activated receptor alpha (PPAR α) for the treatment of a wide range of metabolic disorders. Here, to address the question whether PPAR α agonists can affect the enzymatic activity of 11beta-hydroxysteroid dehydrogenase1 (11β-HSD1), we tested fibrates and WY-14643 for the inhibition of cellular 11β-HSD1 activity in C2C12 myotubes. Only fenofibrate but not fenofibric acid, an active agonist of PPAR α, exerted a potent inhibitory activity in the cell based assay, showing an IC(50) of 1.6 μM. Furthermore, we also demonstrated that the masking of carboxyl group in fenofibric acid via esterification or amidation was required for the inhibitory potencies of fenofibric acid derivatives against 11β-HSD1. In this presentation, we propose that fenofibrate can display a pharmacodynamic role distinct from fenofibric acid through masking of carboxyl group in fenofibric acid.
journal_name
Mol Cell Biochemjournal_title
Molecular and cellular biochemistryauthors
Kim CH,Ramu R,Ahn JH,Bae MA,Cho YSdoi
10.1007/s11010-010-0532-4subject
Has Abstractpub_date
2010-11-01 00:00:00pages
91-8issue
1-2eissn
0300-8177issn
1573-4919journal_volume
344pub_type
杂志文章abstract::Silkworm (Bombyx mori) is not only a model organism for scientific studies, but also a commercial insect for agricultural production. BmAtg8 (a B. mori homolog of yeast Atg8) plays crucial roles in macroautophagy (hereafter referred to autophagy), which is helpful for silkworm metamorphosis. Relevant mechanism about B...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-019-03513-y
更新日期:2019-07-01 00:00:00
abstract::We have examined a possibility whether or not severity and extent of coronary atherosclerosis may associate with degree of local inflammation in relation to endothelial dysfunction as is indicated by reduced NO formation. Blood samples were obtained from aortic root (Ao) and coronary sinus (CS) of 39 patients who unde...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:
更新日期:2003-07-01 00:00:00
abstract::Gastrin has significant growth and metabolic effects on colonic mucosal cells. It is, however, not known if gastrin receptors are present on colonic mucosal cells that may directly mediate the reported biological effects of gastrin. In the present studies, the presence of specific gastrin binding sites on colonic muco...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/BF00227573
更新日期:1992-06-26 00:00:00
abstract::Atherosclerosis is the leading cause of death in North America. It is characterized by thickening of the coronary artery wall by the formation of plaques, resulting in reduced blood flow. Plaque rupture and the consequent thrombosis may lead to sudden blockage of arteries and causing stroke and heart attack. In the la...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章,评审
doi:10.1023/a:1017286006708
更新日期:2000-04-01 00:00:00
abstract::An increasing amount of experimental and epidemiological evidence implicates the involvement of oxygen derived radicals in the pathogenesis of cancer development. It is well known that chemical carcinogenesis is multistage process. Free radicals arefound to be involved in both initiation and promotion of multistage ca...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-005-0325-3
更新日期:2005-05-01 00:00:00
abstract::Increased protein kinase C (PKC) activity has been implicated in the pathogenesis of a number of diabetic complications, and high concentrations of glucose have been shown to increase PKC activity. The present study was designed to examine the role of PKC in diabetes-induced (and glucose-induced) cardiomyocyte dysfunc...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1023/b:mcbi.0000038231.68078.4b
更新日期:2004-07-01 00:00:00
abstract::Syndecan-4 (S4) is a cell membrane heparan sulfate proteoglycan that plays a role in satellite cell mediated myogenesis. S4 modulates the proliferation of myogenic satellite cells, but the mechanism of how S4 functions during myogenesis is not well understood. In other cell systems, S4 has been shown to form oligomers...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-011-1198-2
更新日期:2012-04-01 00:00:00
abstract::Calcineurin inhibitors are used in immunosuppressive therapy applied after transplantation, but they are associated with major metabolic side effects including the development of new onset diabetes. Previously, we have shown that the calcineurin inhibiting drugs tacrolimus and cyclosporin A reduce adipocyte and myocyt...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-017-3261-0
更新日期:2018-08-01 00:00:00
abstract::The mechanism of the effect of beta-hydroxy-beta-methylbutyrate (HMB) on protein degradation induced by lipopolysaccharide (LPS) has been evaluated in murine myotubes. HMB (50 muM) completely attenuated total protein degradation induced by LPS (1-100 ng/ml), formation of reactive oxygen species (ROS) and activation of...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-009-0130-5
更新日期:2009-10-01 00:00:00
abstract::AcMNPV is the first baculovirus to be sequenced and is considered a model of baculovirus. ac154 is a later expression gene in AcMNPV genome and its function is unknown. In this study, we explored the function of Ac154 in AcMNPV infection process in host Sf9 cells. The results showed that Ac154 was distributed in both ...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-019-03631-7
更新日期:2020-01-01 00:00:00
abstract::The present study examined the effect of fenoldopam, a known dopamine-1 receptor (DA1) agonist in order to understand its involvement in the cardiac hypertrophic process. Male Sprague-Dawley rats underwent abdominal aortic constriction (AB) with placement of a suprarenal ligature while sham operated animals served as ...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/BF00926744
更新日期:1995-03-09 00:00:00
abstract::Cardiovascular disease has become the leading cause of death in the world. Metastasis-associated lung adenocarcinoma transcript 1 (MALAT1) plays an important role in cardiovascular disease, such as stroke. However, the role of MALAT1 in hypoxia (HYP)-induced vascular endothelial cells (VECs) remains unclear. In the pr...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-020-03684-z
更新日期:2020-03-01 00:00:00
abstract::Lipids form an essential part of the biomembrane and it is of paramount importance to study their conformational aspects. It is found that the present methods of nomenclature for lipids are totally inadequate for describing these diverse amphipathic molecules. Further the existing methods are incompatible in terms of ...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章,评审
doi:10.1007/BF00228093
更新日期:1989-11-23 00:00:00
abstract::Sarcolemmal Ca2+/Mg2+ ecto-ATPase (Myoglein; MW 180 kD) is a membrane bound enzyme which requires a millimolar concentration of either Ca2+ or Mg2+ for maximal hydrolysis of ATP. The isoelectric point (pI) of the cardiac ecto-ATPase was 5.7. The purified Ca2+/Mg2+ ecto-ATPase from the rat heart sarcolemmal appeared as...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1023/a:1006840523916
更新日期:1998-06-01 00:00:00
abstract::We firstly characterized zinc uptake phenomenon across basolateral membrane vesicles (BLMVs) isolated from normal rat kidney. The process was found to be time, temperature, and substrate concentration dependent, and displayed saturability. Zn(2+) uptake was competitively inhibited in the presence of 2 mM Cd with Ki of...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-006-2676-9
更新日期:2006-02-01 00:00:00
abstract::Sinomenine, a pure alkaloid extract from Sinomenium acutum, has anti-inflammatory and immunoregulatory functions. This study investigated the efficiency and the signalling pathways involved in the effect of sinomenine on vascular smooth muscle cell (VSMC) dedifferentiation in response to platelet-derived growth factor...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-012-1474-9
更新日期:2013-01-01 00:00:00
abstract::MicroRNAs (miRNAs) are small non-coding RNAs that have been suggested to play an essential role in tumorigenesis. Reduced expression of miR-338 has been reported in several types of cancers; however, the role of miR-338 in oral squamous cell carcinoma (OSCC) has not been elucidated. In this study, we demonstrated that...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-014-2211-3
更新日期:2015-01-01 00:00:00
abstract::The influence of hypotonic solution on cell volume and electrophysiology properties of the failing heart of cardiomyopathic hamsters (TO-2) was investigated. The results showed an increase in cell volume of quiescent isolated ventricular myocytes by 66% within 30 min. Angiotensin (1-7) [Ang (1-7)] (10(-8) M) administe...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-009-0135-0
更新日期:2009-10-01 00:00:00
abstract::Renilla luciferase reporter is a widely used internal control in dual luciferase reporter assay system, where its transcription is driven by a constitutively active promoter. However, the authenticity of the Renilla luciferase response in some experimental settings has recently been questioned. Testicular receptor 4 (...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-017-2961-9
更新日期:2017-06-01 00:00:00
abstract::Cultured human and rat endothelial cells were used to study cellular toxicity and Ca2+ signalling upon exposure to reactive oxygen species. Superoxide and hydrogen peroxide (O2.-/H2O2) were produced by the hypoxanthine/xanthine oxidase system (HX/XO) and caused intracellular Ca2+ concentration ([Ca2+]i) to rise steadi...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1023/a:1006886215193
更新日期:1997-06-01 00:00:00
abstract::Glucocorticoid hormones (GCH) are anti-inflammatory and immunosuppressive agents that inhibit T-cell growth and activation. Since the T-cell receptor (TCR)/CD3 complex mediates T-lymphocyte activation, we studied the effect of in vitro dexamethasone (DEX), a synthetic GCH, on TCR/CD3 expression. DEX-treatment of a hyb...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1023/a:1006829421509
更新日期:1997-02-01 00:00:00
abstract::Biochemical and structural changes occurring in the myocardium with aging are mainly resulting from the association of a general tissue atrophy with the hypertrophy of the remaining myocytes. Whilst hypertrophy seems to be a compensatory process to the loss of cardiomyocytes and to a mild systolic hypertensive conditi...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章,评审
doi:10.1007/BF00240046
更新日期:1996-07-01 00:00:00
abstract::The manganese superoxide dismutase (MnSOD) ala16val polymorphism has been associated with various diseases including breast cancer. In the present study, we investigated levels of MnSOD protein, enzymatic activity, and mRNA with respect to MnSOD genotype in several human breast carcinoma cell lines and in mouse embryo...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-009-0247-6
更新日期:2010-02-01 00:00:00
abstract::Radioprotection by an aqueous extract of Podophyllum hexandrum (RP-1) was investigated in HepG2 cells by evaluating colony forming efficacy (CFE), redox status of mitochondria, reactive oxygen species (ROS), generation of nitric oxide (NO), peroxidation of lipids and intracellular glutathione. Lower concentrations of ...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1023/a:1024925612233
更新日期:2003-08-01 00:00:00
abstract::Modification of 60S ribosomal subunits from rat liver with dimethylmaleic anhydride (60 mumols/ml) is accompanied by release of 35% of the protein. The acidic ribosomal proteins, as well as 9 basic proteins, are selectively liberated from the ribosomal subunits. Reconstitution of the protein-deficient particles with t...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/BF00218133
更新日期:1990-02-09 00:00:00
abstract::The normal translocation of nascent polypeptides into the lumen of the endoplasmic reticulum (ER) is thought to be aided in part by a translocon-associated protein (TRAP) complex consisting of 4 protein subunits. The association of mature proteins with the ER and Golgi, or other intracellular locales, such as lysosome...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1023/a:1026598516681
更新日期:2000-12-01 00:00:00
abstract::In the eluted fractions of histone-treated crude extracts separated by Sephadex G-200 filtration, multiple protein kinase (PK) activities, including three from brain and two from skeletal muscle, were augmented by both S-100 protein and parvalbumin on the phosphorylation of endogenous substrates. One additional PK act...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/BF00219324
更新日期:1986-06-01 00:00:00
abstract::Endothelial dysfunction (ED) has a high incidence in chronic kidney disease (CKD) and is identified as a precursor to cardiovascular events. Recent studies suggest that leptin may be the missing link between ED and CKD. The objective of this study was to investigate the mechanism by which leptin causes ED and the conn...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/s11010-020-03816-5
更新日期:2020-10-01 00:00:00
abstract::The subcellular distribution and substrate kinetics of soluble and particulate-associated bovine adrenal glycerol kinase have been investigated. Whole adrenal, adrenal cortex and adrenal medulla were examined for distribution of glycerol kinase between soluble and particulate fractions. No major differences in distrib...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1007/BF00420928
更新日期:1984-09-01 00:00:00
abstract::Glomerular mesangial cells play an important role in the development of glomerulosclerosis. Mesangial cell apoptosis has been shown to be involved in different stages of development of glomerulonephritis. The aim of the present study was to evaluate the effect of inhibition of serine/threonine phosphatases by okadaic ...
journal_title:Molecular and cellular biochemistry
pub_type: 杂志文章
doi:10.1023/b:mcbi.0000026041.41078.32
更新日期:2004-05-01 00:00:00