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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
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
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
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
Tony K L Kiang et al.
Pharmacology & therapeutics, 106(1), 97-132 (2005-03-23)
UDP-glucuronosyltransferase (UGT) enzymes catalyze the conjugation of various endogenous substances (e.g., bilirubin) and exogenous compounds (e.g., drugs). The human UGT superfamily is comprised of 2 families (UGT1 and UGT2) and 3 subfamilies (UGT1A, UGT2A, and UGT2B). Many of the individual
Ayhan Yaman et al.
Pediatric emergency care, 29(5), 659-661 (2013-05-04)
Valproic acid (VPA) is still an important antiepileptic drug, with the broadest spectrum used in all types of seizures and syndromes. It has serious adverse effects such as hepatotoxicity, hyperammonemic encephalopathy, coagulation disorders, and pancreatitis. The incidence of VPA-associated pancreatitis
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
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
Henry F Duncan et al.
Experimental cell research, 319(10), 1534-1543 (2013-04-09)
Application of histone deacetylase inhibitors (HDACi) to cells epigenetically alters their chromatin structure and induces transcriptional and cellular reparative events. This study investigated the application of two HDACi, valproic acid (VPA) and trichostatin A (TSA) on the induction of repair-associated
Long-term follow-up for efficacy and safety of treatment of retinitis pigmentosa with valproic acid.
Sheena Bhalla et al.
The British journal of ophthalmology, 97(7), 895-899 (2013-04-23)
The purpose of this study was to determine the long-term efficacy and safety of valproic acid (VPA) treatment in patients with pigmentary retinal dystrophies. A retrospective chart review was conducted on 31 patients with a diagnosis of pigmentary retinal dystrophy
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
Andrea Cipriani et al.
The Cochrane database of systematic reviews, 10(10), CD003196-CD003196 (2013-10-18)
Bipolar disorder is a recurrent illness that is amongst the top 30 causes of disability worldwide and is associated with significant healthcare costs. In the past, emphasis was placed solely on the treatment of acute episodes of bipolar disorder; recently
R Scott Obach et al.
Drug metabolism and disposition: the biological fate of chemicals, 36(7), 1385-1405 (2008-04-23)
We present herein a compilation and trend analysis of human i.v. pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data. This data set provides the drug metabolism scientist with a
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
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
Systematic Review of Randomized Clinical Trials on Safety and Efficacy of Pharmacological and Nonpharmacological Treatments for Retinitis Pigmentosa.
Marta Sacchetti et al.
Journal of ophthalmology, 2015, 737053-737053 (2015-09-05)
Zhi-Feng Xie et al.
Bioorganic & medicinal chemistry letters, 15(21), 4803-4805 (2005-09-06)
A series of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline derivatives was synthesized using 6-hydroxy-3,4-dihydro-1H-quinolin-2-one as a starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES test) and the subcutaneous (s.c.) pentylenetetrazol test (scMet test), and their neurotoxicity was evaluated by 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
S Eyal et al.
British journal of pharmacology, 149(3), 250-260 (2006-08-09)
The antiepileptic drug valproic acid, a histone deacetylase (HDAC) inhibitor, is currently being tested as an anticancer agent. However, HDAC inhibitors may interact with anticancer drugs through induction of P-glycoprotein (P-gp, MDR1) expression. In this study we assessed whether valproic
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
Yuanyuan Shi et al.
Bioorganic & medicinal chemistry letters, 17(16), 4491-4494 (2007-06-15)
Valproic (2-propylpentanoic) acid is a commonly used drug in the treatment of bipolar disorder and epilepsy. The molecular mechanism that underlies its clinical efficacy remains controversial and is complicated by the broad range of intracellular effects of valproic acid, including
Histone deacetylase inhibitor, 2-propylpentanoic acid, increases the chemosensitivity and radiosensitivity of human glioma cell linesin vitro
Cuijie S, et al.
Chinese Medical Journal (English Edition), 125(24), 4338-4343 (2012)
Pityriasis rosea-like eruption associated with lamotrigine.
Evangelia Papadavid et al.
Journal of the American Academy of Dermatology, 68(6), e180-e181 (2013-05-18)
Camelia Musleh et al.
Neurology, 81(18), e130-e134 (2013-10-30)
A 16-year-old right-handed boy presented for consultation for recent development of seizures. He is the product of a normal pregnancy and delivery without a history of developmental delay, head trauma, or family history of epilepsy. A year and a half
Jian Wang et al.
Cancer biology & therapy, 15(9), 1198-1207 (2014-06-12)
HPP1 (hyperplastic polyposis protein 1), a tumor suppressor gene, is downregulated by promoter hypermethylation in a number of tumor types including colon cancer. c-Myc is also known to play a role in the suppression of HPP1 expression via binding to
Sharon Berendsen et al.
Expert opinion on investigational drugs, 21(9), 1391-1415 (2012-06-07)
Glioblastoma multiforme is the most common and aggressive primary brain tumor. Valproate has been used as an anti-epileptic drug and mood stabilizer for decades. Recently, it was found to inhibit the proliferation of various cancers including glioblastoma multiforme. We provide
Miki Yuyama et al.
The Biochemical journal, 459(3), 489-503 (2014-02-12)
VPA (valproic acid), a short-chain fatty acid that is a HDAC (histone deacetylase) inhibitor, is known to suppress adipogenesis. In the present study, we identified the molecular mechanism of VPA-mediated suppression of adipogenesis in adipocytes. VPA suppressed the accumulation of
Roman Tyzio et al.
Science (New York, N.Y.), 343(6171), 675-679 (2014-02-08)
We report that the oxytocin-mediated neuroprotective γ-aminobutyric acid (GABA) excitatory-inhibitory shift during delivery is abolished in the valproate and fragile X rodent models of autism. During delivery and subsequently, hippocampal neurons in these models have elevated intracellular chloride levels, increased
Nigel Greene et al.
Chemical research in toxicology, 23(7), 1215-1222 (2010-06-18)
Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential
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