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P6273
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Ji-Young Choi et al.
Biochemical and biophysical research communications, 450(1), 372-377 (2014-06-19)
Glutamate carboxypeptidase II (GCPII) is known to be implicated in brain diseases such as schizophrenia and bipolar disorder, and dramatically increases in prostate cancer. Here, we investigated the regulation of GCPII expression in astrocytes and examined whether GCPII is epigenetically
Mike De Vrieze et al.
Analytical and bioanalytical chemistry, 406(25), 6179-6188 (2014-08-16)
Over the past decades, several in vitro methods have been tested for their ability to predict drug penetration across the blood-brain barrier. So far, in high-performance liquid chromatography, most attention has been paid to micellar liquid chromatography and immobilized artificial
Inge M Westra et al.
Toxicology and applied pharmacology, 274(2), 328-338 (2013-12-11)
Induction of fibrosis during prolonged culture of precision-cut liver slices (PCLS) was reported. In this study, the use of rat PCLS was investigated to further characterize the mechanism of early onset of fibrosis in this model and the effects of
Takeki Uehara et al.
Molecular nutrition & food research, 54(2), 218-227 (2009-12-31)
Biotechnology advances have provided novel methods for the risk assessment of chemicals. The application of microarray technologies to toxicology, known as toxicogenomics, is becoming an accepted approach for identifying chemicals with potential safety problems. Gene expression profiling is expected to
Hang-Soo Park et al.
Biomaterials, 39, 47-58 (2014-12-06)
The generation of induced pluripotent stem cells (iPSCs) often causes genetic and epigenetic defects, which may limit their clinical applications. Here, we show that reprogramming in the presence of small molecules preserved the genomic stability of iPSCs by inhibiting DNA
Oday Alsarraf et al.
Experimental eye research, 127, 124-131 (2014-07-30)
Neuroretinal ischemic injury contributes to several degenerative diseases in the eye and the resulting pathogenic processes involving a series of necrotic and apoptotic events. This study investigates the time and extent of changes in acetylation, and whether this influences function
Fernando Dueñas et al.
BMC veterinary research, 10, 154-154 (2014-07-12)
Mesenchymal stem cells (MSC) are multipotent progenitor cells characterized by their ability to both self-renew and differentiate into tissues of mesodermal origin. The plasticity or transdifferentiation potential of MSC is not limited to mesodermal derivatives, since under appropriate cell culture
Hideki Mutai et al.
PloS one, 10(4), e0124301-e0124301 (2015-04-16)
Various factors that are important for proper hearing have been identified, including serum levels of zinc. Here we investigated whether epigenetic regulatory pathways, which can be modified by environmental factors, could modulate hearing. RT-PCR detected expression of genes encoding DNA
Jianguo Wang et al.
The Journal of biological chemistry, 282(39), 28408-28418 (2007-08-07)
Histone deacetylase inhibitors (HDACi), such as trichostatin A (TSA), can regulate gene expression by promoting acetylation of histones and transcription factors. Human tissue factor (TF) expression is partly governed by a unique, NF-kappaB-related "TF-kappaB" promoter binding site. We find that
Andrea Williams et al.
Nature chemical biology, 4(5), 295-305 (2008-04-09)
Autophagy is a major clearance route for intracellular aggregate-prone proteins causing diseases such as Huntington's disease. Autophagy induction with the mTOR inhibitor rapamycin accelerates clearance of these toxic substrates. As rapamycin has nontrivial side effects, we screened FDA-approved drugs to
Tiago L Moda et al.
Bioorganic & medicinal chemistry, 15(24), 7738-7745 (2007-09-18)
A drug intended for use in humans should have an ideal balance of pharmacokinetics and safety, as well as potency and selectivity. Unfavorable pharmacokinetics can negatively affect the clinical development of many otherwise promising drug candidates. A variety of in
Simone E Dekker et al.
The Journal of surgical research, 190(1), 312-318 (2014-04-04)
We have previously shown that resuscitation with fresh frozen plasma (FFP) in a large animal model of traumatic brain injury (TBI) and hemorrhagic shock (HS) decreases the size of the brain lesion, and that addition of a histone deacetylase inhibitor
Xiaofei Li et al.
Biochemical and biophysical research communications, 436(2), 259-264 (2013-06-04)
Aspirin and valproic acid (VPA) have been extensively studied for inducing various malignancies growth inhibition respectively, despite their severe side effects. Here, we developed a novel combination by aspirin and VPA on hepatocellular cancer cells (HCCs). The viability of HCC
Wolfgang Löscher
CNS drugs, 16(10), 669-694 (2002-09-25)
Since its first marketing as an antiepileptic drug (AED) 35 years ago in France, valproate has become established worldwide as one of the most widely used AEDs in the treatment of both generalised and partial seizures in adults and children.
Terina N Martinez et al.
Molecular neurodegeneration, 7, 45-45 (2012-09-15)
Dopaminergic (DA) neurons in the ventral midbrain selectively degenerate in Parkinson's disease (PD) in part because their oxidative environment in the substantia nigra (SN) may render them vulnerable to neuroinflammatory stimuli. Chronic inhibition of soluble Tumor Necrosis Factor (TNF) with
Akihiko Machino et al.
Hiroshima journal of medical sciences, 62(1), 7-12 (2013-04-23)
The appropriate therapeutic serum valproate level in maintenance therapy for bipolar disorder is not well known. We studied the serum valproate levels in seventeen bipolar I and twenty-four bipolar II disorder outpatients who had been treated with stable doses of
Jakob Avi Shimshoni et al.
Journal of medicinal chemistry, 50(25), 6419-6427 (2007-11-13)
Valproic acid (VPA) is a major antiepileptic drug (AED); however, its use is limited by two life-threatening side effects: teratogenicity and hepatotoxicity. Several constitutional isomers of VPA and their amide and urea derivatives were synthesized and evaluated in three different
Bilegtsaikhan Tsolmongyn et al.
Cellular immunology, 282(2), 100-105 (2013-06-19)
The effect of lipopolysaccharide (LPS) on valproic acid (VPA)-induced cell death was examined by using mouse RAW 264.7 macrophage cells. LPS inhibited the activation of caspase 3 and poly (ADP-ribose) polymerase and prevented VPA-induced apoptosis. LPS inhibited VPA-induced p53 activation
Koji Sugimoto et al.
Anticancer research, 34(7), 3403-3409 (2014-07-02)
Valproic acid (VPA) acts as a specific inhibitor of class I HDACs and it use has been proven to be safe since a long time. In the present study, we investigated the effect of VPA in the combination with pegylated
Martina Korfei et al.
Thorax, 70(11), 1022-1032 (2015-09-12)
Activation and differentiation of fibroblasts into contractile protein-expressing myofibroblasts and their acquired apoptosis-resistant phenotype are critical factors towards the development of idiopathic pulmonary fibrosis (IPF), a fatal disease characterised by distorted pulmonary structure and excessive extracellular matrix (ECM) deposition. The
Maria Lyngaas Torgersen et al.
Blood, 122(14), 2467-2476 (2013-08-24)
The role of autophagy during leukemia treatment is unclear. On the one hand, autophagy might be induced as a prosurvival response to therapy, thereby reducing treatment efficiency. On the other hand, autophagy may contribute to degradation of fusion oncoproteins, as
J Fisher et al.
Clinical toxicology (Philadelphia, Pa.), 52(1), 63-65 (2013-12-25)
Methylene blue inhibits the nitric oxide-cyclic guanosine monophosphate (NO-cGMP) pathway, decreasing vasodilation and increasing responsiveness to vasopressors. It is reported to improve haemodynamics in distributive shock from various causes including septicaemia and post-cardiac surgery. Reports of use in overdose are
Michael H Abraham et al.
European journal of medicinal chemistry, 43(3), 478-485 (2007-06-05)
Values of in vitro gas to lung partition coefficients, K(lung), of VOCs have been collected from the literature. For 44 VOCs, application of the Abraham solvation equation to log K(lung) yielded a correlation with R(2)=0.968 and S.D.=0.25 log units. Combination
Yue Zhang et al.
Biochemical and biophysical research communications, 450(1), 433-439 (2014-06-10)
HDAC6 is a major cytoplasmic deacetylase. XBP1s is a basic-region leucine zipper (bZIP) transcriptional factor. Despite their mutual involvement in the anti-oxidative process, there are no reports about their inter-protein interactions so far. Here we identified a direct link between
L A Gromov et al.
Ukrains'kyi biokhimichnyi zhurnal (1999 ), 85(1), 79-83 (2013-03-29)
The effect of phenobarbital, carbamazepine, valproate sodium, depakine, topiramate and lamotrigine on the content of NO and NO-synthase activity in white rat brain tissues has been studied. It was established that the action of carbamazepine, valproate sodium, topiramate and lamotrigine
Laura Cervera et al.
Applied microbiology and biotechnology, 99(23), 9935-9949 (2015-08-19)
The manufacturing of biopharmaceuticals in mammalian cells typically relies on the use of stable producer cell lines. However, in recent years, transient gene expression has emerged as a suitable technology for rapid production of biopharmaceuticals. Transient gene expression is particularly
Jennifer A Corcoran et al.
PLoS pathogens, 11(1), e1004597-e1004597 (2015-01-09)
Kaposi's sarcoma-associated herpesvirus (KSHV) is the infectious cause of several AIDS-related cancers, including the endothelial cell (EC) neoplasm Kaposi's sarcoma (KS). KSHV-infected ECs secrete abundant host-derived pro-inflammatory molecules and angiogenic factors that contribute to tumorigenesis. The precise contributions of viral
Response to letter regarding article, “histone deacetylation inhibition in pulmonary hypertension: therapeutic potential of valproic acid and suberoylanilide hydroxamic acid”.
Lan Zhao et al.
Circulation, 127(14), e540-e540 (2013-05-22)
Anton Pohanka et al.
Scandinavian journal of clinical and laboratory investigation, 74(7), 648-652 (2014-07-26)
Therapeutic drug monitoring (TDM) of the antiepileptic drug valproic acid (VPA) is recommended in patients with multiple drug therapy or with concomitant disabilities to ensure treatment efficacy and avoid adverse reactions in both adults and children. The use of sampling
Yun W Alelyunas et al.
Bioorganic & medicinal chemistry letters, 20(24), 7312-7316 (2010-11-09)
We determined the experimental solubility of CNS marketed drugs. Of the 98 drugs measured, greater than 90% had solubility >10 μM in pH 7.4 buffer. Only seven drugs had solubility <10 μM. Using these data, we established a solubility criterion
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