Find your PDFs fast.
Welcome to the Pubget Medical Subject Headings (MESH) browser. Click on a topic or subtopic below to explore related papers. In the gold box is the most recent paper about the current MESH term, and below are 20 related papers.
Pyrazoles (8):
Recent article
Pyrazoles
Abstract
We continued the double-masked ADAPT protocol for 2 additional years to investigate incidence of AD (primary outcome). We then collected cerebrospinal fluid (CSF) from 117 volunteer participants to assess their ratio of CSF tau to Aβ(1-42.)
Including 40 new events observed during fo...
|
PMID: 21784351
PDF is available here.
PDF is available here.
| < More recent | Older article > |
Abstract
The primary objective of this study was to determine the rate of pathological response after preoperative celecoxib and concurrent taxane-based chemotherapy in patients with cancer of the esophagus and gastroesophageal junction.
Thirty-nine patients were enrolled in t...
|
PMID: 21532508
PDF is available here.
PDF is available here.
Abstract
Abstract
We investigated whether metformin inhibits the release of HMGB1 in LPS-treated RAW 264.7 cells and increases survival rate in endotoxaemic mice (lethal endotoxaemia was induced by an i.p. injection of LPS). This was achieved by a range of techniques including Western blotting, enzyme-linked immunoso...
|
PMID: 21091653
PDF is available here.
PDF is available here.
Abstract
We investigated the effects of a novel small-molecule JAK inhibitor (AZD1480) on IL-6/JAK signal transduction and its biological consequences on the human myeloma-derived cell lines U266 and Kms.11. At low micromolar concentrations, AZD1480 blocks cell proliferation and induces apoptosis of myeloma...
|
PMID: 21164517
PDF is available here.
PDF is available here.
Abstract
Abstract
Abstract
Abstract
Abstract
The discovery of JAK2V617F has rejuvenated interest in Janus kinase (JAK)-signal transducer and activator of transcription (STAT), both as an oncogenic pathway and a drug target in BCR-ABL1-negative myeloproliferative neoplasms (MPN). However, the complexity of these diseases in term...
|
PMID: 21079613
PDF is available here.
PDF is available here.
Abstract
Traditional treatment of primary (idiopathic) immune thrombocytopenia (ITP) predominantly consists of immune suppression and/or modulation. In addition, many treated patients develop severe adverse effects, and approximately a third of patients do not respond. Two of the newly develo...
|
PMID: 21322783
PDF is available here.
PDF is available here.
Abstract
We speculate that treatment with celecoxib may, in some instances, enhance tumor cell expression of VEGF as well as angiogenesis and, consequently, may have detrimental effects on the response of tumors to this drug.
©2010 AACR....
|
PMID: 21220497
PDF is available here.
PDF is available here.
Abstract
We conducted this pilot study to evaluate the effect of rimonabant on body weight and composition of adults with PWS.
This was a double blind placebo controlled study. Body weight, total fat mass, fasting ghrelin, leptin, IGF1 and insulin like growth factor binding protein (IGFBP-3)...
|
PMID: 20965292
PDF is available here.
PDF is available here.
Abstract
We investigated the effect of the antiobesity drug SR141716 (a CB1 antagonist) on macrophage-mediated inhibition of insulin signaling in adipocytes. THP1 macrophages (THP1) were stimulated in vitro with lipopolysaccharide (LPS) and SR141716 or vehicle. The resulting conditioned medium (CM) was analy...
|
PMID: 20379144
PDF is available here.
PDF is available here.
Abstract
Adult T-cell leukemia/lymphoma (ATL) is a highly aggressive disease in which the Jak2/Stat5 pathway is constitutively activated. This study found that AZ960, a novel inhibitor of Jak2 kinase, effectively induced growth arrest and apoptosis of human T-cell lymphotropic virus type 1, H...
|
PMID: 21159615
PDF is available here.
PDF is available here.
Abstract
Adult T-cell leukemia/lymphoma (ATL) is a highly aggressive disease in which the Jak2/Stat5 pathway is constitutively activated. This study found that AZ960, a novel inhibitor of Jak2 kinase, effectively induced growth arrest and apoptosis of human T-cell lymphotropic virus type 1, H...
|
PMID: 21159615
PDF is available here.
PDF is available here.
Abstract
The synthesis and full characterization of new half-sandwich ruthenium(II) complexes containing κ(3)(N,N,N)-hydridotris(pyrazolyl)borate (κ(3)(N,N,N)-Tp) and the water-soluble phosphanes 1,3,5-triaza-7-phosphatricyclo[3.3.1.1(3,7)]decane (PTA) and 1-methyl-3,5-diaza-1-azonia-7-phosphatricyclo[3.3....
|
PMID: 20882255
PDF is available here.
PDF is available here.
Brain research (1360) 2010
Abstract
We investigated whether or not the extracellular signal regulated-kinase 1/2 (ERK1/2) pathway was involved in the ischemic tolerance induced by EA pretreatment through CB1R. At 24h after the end of the last EA pretreatment, focal cerebral ischemia was induced by middle cerebral artery occlusion for...
|
PMID: 20654595
PDF is available here.
PDF is available here.
Abstract
We evaluated whether LTB4 was involved in celecoxib-mediated inhibitory effect on human colon cancer HT-29 cells and human prostate cancer PC-3 cells. Our data showed that survival of both cell lines was obviously suppressed after celecoxib treatment for 72 h in a concentration-dependent manner. How...
|
PMID: 20937254
PDF is available here.
PDF is available here.
Abstract
We report the identification of a pyrazolo[1,5-a]pyrimidine derived compound, 4k (BS-194), as a selective and potent CDK inhibitor, which inhibits CDK2, CDK1, CDK5, CDK7, and CDK9 (IC₅₀= 3, 30, 30, 250, and 90 nmol/L, respectively). Cell-based studies showed inhibition of the phosphorylation of...
|
PMID: 21080703
PDF is available here.
PDF is available here.
Abstract
We show here that the converse also holds true: the conformational state of the estrogen receptor can direct distinct orientations of the bound ligand. 'Gain-of-allostery' mutations that mimic the effects of ligand in driving protein conformation allowed crystallization of the partial agonist ligand...
|
PMID: 20924370
PDF is available here.
PDF is available here.
Abstract
The most frequent cardiac arrhythmia and main cause for cardio-embolic stroke is atrial fibrillation. Prophylaxis for thrombembolic events is performed regarding individual risk of patients with either ASS or vitamin-K-antagonists. Efficacy and safety of oral anticoagulation is limited by a narrow t...
|
PMID: 21064013
PDF is available here.
PDF is available here.
Abstract
CC chemokine receptor 1 (CCR1) is a GPCR involved in the migration and activation of leukocytes. A number of studies have highlighted a role for CCR1 in preclinical animal models of inflammatory diseases, including MS and rheumatoid arthritis.
This review examines three reports on a new series of CC...
|
PMID: 20858032
PDF is available here.
PDF is available here.
Acta Pharmacologica Sinica (31)11 2010
Abstract
To investigate whether rimonabant, a cannabinoid receptor antagonist, had inhibitory effects on inflammatory reactions in human umbilical vein endothelial cells (HUVEC).
TNF-α-induced IL-6 production was measured by ELISA and effects on related signaling pathways wer...
|
PMID: 20953204
PDF is available here.
PDF is available here.
Cellular Signalling (22)11 2010
Abstract
We observed that AMPK-alpha can be activated by transforming growth factor-beta1 (TGF-beta1) in mouse hepatocytes. Inhibition of AMPK by Compound C, a selective AMPK-alpha inhibitor, inhibited TGF-beta1-induced apoptosis and EMT in hepatocytes. In addition, overexpression of a dominant-negative form...
|
PMID: 20650315
PDF is available here.
PDF is available here.
Arthritis & Rheumatism (62)11 2010
Abstract
The activity of p38 MAPK regulates lipopolysaccharide (LPS)-stimulated production of key proinflammatory cytokines such as tumor necrosis factor α (TNFα). Consequently, p38 MAPK inhibitors have attracted considerable interest as potential treatments of rheumatoid arthritis (RA), and studies in mur...
|
PMID: 20589681
PDF is available here.
PDF is available here.
Neuroscience (170)2 2010
Abstract
Our recent study has shown that it may inhibit cyclooxygenase-2 (COX-2) in the spinal dorsal horn where COX-2 is upregulated after the development of neuropathic pain following spinal nerve ligation (SNL). The current study directly compared the effect of acupuncture with COX-2 inhibitor celecoxib i...
|
PMID: 20654703
PDF is available here.
PDF is available here.
Abstract
We evaluated body weight, adiposity, liver histology, and hepatic triglyceride content in high-fat diet (HFD)-fed C57BL/6J mice treated with NDGA. In addition, we characterized the underlying mechanism of NDGA's effects in HepG2 hepatocytes by Western blot and RT-PCR analysis. NDGA (100 or 200mg/kg/...
|
PMID: 20836990
PDF is available here.
PDF is available here.
Abstract
We examined effects on some biochemical parameters and kidney and liver tissues of celecoxib-treated Wistar albino male rats. At the end of the study, hepatic and renal function tests were performed and liver and kidney of rats were microscopically examined to detect systemic toxicity of celecoxib....
|
PMID: 20121624
PDF is available here.
PDF is available here.
Abstract
Reducing smoking is a chief priority for governments and health systems like the UK National Health Service (NHS). The UK has implemented a comprehensive tobacco control strategy involving a combination of population tobacco control interventions combined with treatment for dependent smokers through...
|
PMID: 21040645
PDF is available here.
PDF is available here.
Abstract
We initiated a randomised controlled pre-surgical study of celecoxib versus no treatment in women with primary breast cancer to determine the effects of COX-2 inhibition on markers of biological response. Postmenopausal women (50-80 years of age) with stage I or II, primary breast cancer, were rando...
|
PMID: 20697803
PDF is available here.
PDF is available here.
Anticancer Research (30)10 2010
Abstract
Our results indicate that angiosarcoma cell proliferation can be inhibited by subtoxic doses of rapamycin and celecoxib. Due to their direct and stroma-mediated anticancer activities, mTOR antagonists and COX2 inhibitors represent very promising drugs in the palliative treatment of angiosarcoma....
|
PMID: 21036716
PDF is available here.
PDF is available here.
Abstract
We show that apoptosis signal-regulating kinase 1(-/-) (ASK1 KO) mice were resistant to inflammatory arthritis induced in the K/BxN serum transfer model of rheumatoid arthritis (RA). The p38 inhibitor, SD-0006 was administered to wild type (WT) mice as a comparator. Both ASK1 KO and p38 inhibition r...
|
PMID: 20609399
PDF is available here.
PDF is available here.
Abstract
We have evaluated a novel cannabinoid antagonist (AM6545) designed to have limited CNS penetration, to see if it would inhibit food intake in rodents, without aversive effects.
Cannabinoid receptor binding studies, cAMP assays, brain penetration studies and gastrointestinal motility studies were car...
|
PMID: 20880401
PDF is available here.
PDF is available here.
Clinical calcium (20)10 2010
Abstract
Fibrodysplasia ossificans progressiva (FOP) is a rare autosomal dominant disorder characterized by progressive heterotopic bone formation in skeletal muscle tissue. In 2007, FOP was authorized as one of the Intractable Disorders by the Ministry of Health, Labour and Welfare of Japan. The Research Co...
|
PMID: 20890033
PDF is available here.
PDF is available here.
Abstract
The synthesis and Zn(2+) coordination properties of a new macrocycle (L1) obtained by dipodal (2 + 2) condensation of the polyamine 3-(naphthalen-2-ylmethyl)pentane-1,5-diamine with 1H-pyrazole-3,5-dicarbaldehyde are reported. pH-metric studies show that L1 bears five measurable protonation steps in...
|
PMID: 20661509
PDF is available here.
PDF is available here.
Abstract
Firocoxib and meloxicam administration resulted in a lower plasma PGE2 concentration than at baseline on days 3 and 8 of administration, whereas tepoxalin administration did not. Tepoxalin administration resulted in a lower serum TXB2 concentration and pyloric and duodenal PGE1 synthesis on both day...
|
PMID: 20807147
PDF is available here.
PDF is available here.
Abstract
Expenditures on prescribed drugs in Canada are now well past those for all services provided by outpatient physicians ($26.9 billion vs. $21.5 billion in 2007). Government has the opportunity to dedicate resources to continuing medical education of physicians, and effective profiling would assist in...
|
PMID: 20813338
PDF is available here.
PDF is available here.
The Lancet (376)9740 2010
Abstract
The Lancet (376)9740 2010
Abstract
At a mean follow-up of 13.8 months (95% CI 13.6-14.0), the trial was prematurely discontinued because of concerns by health regulatory authorities in three countries about suicide in individuals receiving rimonabant. All randomised participants were analysed. At the close of the trial (Nov 6, 2008),...
|
PMID: 20709233
PDF is available here.
PDF is available here.
Abstract
These results suggest that compound 35 may serve as a promising agent for further development in the treatment of glaucoma....
|
PMID: 20684608
PDF is available here.
PDF is available here.
Abstract
We herein report the discovery of a series of potent and selective serotonin 5-HT(2A) receptor antagonists based on a phenethylpiperazine amide core structure. When tested in a rat sleep pharmacology model, these compounds increased both sleep consolidation and deep sleep. Within this series of comp...
|
PMID: 20684606
PDF is available here.
PDF is available here.
Abstract
We explore the role of surface glycoprotein receptors and signaling proteins in regulating MK migration and platelet recovery after immune-induced thrombocytopenia. We show that spreading and migration of mouse primary bone marrow-derived MKs on a fibronectin matrix are abolished by the Src family k...
|
PMID: 20457868
PDF is available here.
PDF is available here.
Abstract
We show that the novel small-molecule PHA-848125, a potent dual inhibitor of CDKs and TRKs, possesses significant antitumor activity. The compound inhibits cell proliferation of a wide panel of tumoral cell lines with submicromolar IC(50). PHA-848125-treated cells show cell cycle arrest in G(1) and...
|
PMID: 20682657
PDF is available here.
PDF is available here.
Abstract
We hypothesized that T-H induces PP T cell dysfunction and E2 administration following T-H will improve PP T cell function. T-H was induced in male C3H/HeN mice (6-8weeks) by midline laparotomy and approximately 90min of hemorrhagic shock (blood pressure 35mmHg), followed by fluid resuscitation (4x...
|
PMID: 20400328
PDF is available here.
PDF is available here.
Abstract
The combined use of two-dimensional NMR correlation experiments and gauge including atomic orbital density functional theory in (13)C NMR chemical shift (CS) calculations allowed reliable and simple structural determination of regioisomeric heterocyclic systems that originate from the reactions of a...
|
PMID: 20589725
PDF is available here.
PDF is available here.
Abstract
We aimed to investigate the effects of new NO/cyclic guanosine monophosphate (cGMP) pathway-affecting agents at the sheep sphincter of Oddi (SO) in vitro.
Sheep SO rings were mounted in organ baths and tested for isometric tension and cGMP levels in response to 3,3-bis(aminoethyl)-1-hydroxy-2-oxo-1-...
|
PMID: 20697210
PDF is available here.
PDF is available here.
Abstract
The intraoperatively fentayl requirement were similar among the three groups (p < 0.00). Celecoxib and parecoxib significantly decreased the amount of morphine requirement after total hip or knee arthroplasty compared to placebo at 1, 6, 12 and 24 hours (p < 0.00). The celecoxib group required more...
|
PMID: 20718170
PDF is available here.
PDF is available here.
Abstract
We have demonstrated that a CB1R neutral antagonist largely restricted to the periphery does not affect behavioral responses mediated by CB1R in the brains of mice with genetic or diet-induced obesity, but it does cause weight-independent improvements in glucose homeostasis, fatty liver, and plasma...
|
PMID: 20664173
PDF is available here.
PDF is available here.
Journal of Hypertension (28)8 2010
Abstract
In both animal models, riociguat treatment improved survival and normalized blood pressure. Moreover, in the L-NAME study part, riociguat reduced cardiac target organ damage as indicated by lower plasma ANP, lower relative left ventricular weight and lower cardiac interstitial fibrosis, and reduced...
|
PMID: 20613628
PDF is available here.
PDF is available here.
Thrombosis and Haemostasis (104)2 2010
Abstract
Apixaban is an oral, direct and highly selective factor Xa (FXa) inhibitor in late-stage clinical development. This study evaluated the in vitro effect of apixaban on human platelet aggregation induced by thrombin derived via the extrinsic pathway. Direct inhibitors of FXa (rivaroxaban), FVIIa (BMS-5...
|
PMID: 20589316
PDF is available here.
PDF is available here.
Abstract
To investigate whether AMP-activated protein kinase (AMPK) regulates the expression of pancreatic duodenal homeobox-1 (PDX-1), a beta-cell-specific transcription factor and whether PPARalpha/gamma is involved in the regulation of pancreatic beta-cell lines after acute stimulation....
|
PMID: 20644547
PDF is available here.
PDF is available here.
Bioresource Technology (101)15 2010
Abstract
This study focused on the competitive biosorption of Yellow 2G (Y2G) and Reactive Brilliant Red K-2G (RBR) by inactive aerobic granules in binary solutions. A first-order derivative spectrophotometric method for the simultaneous determination of Y2G and RBR in binary solutions was developed. Dubinin...
|
PMID: 20303747
PDF is available here.
PDF is available here.
Inorganic Chemistry (49)15 2010
Abstract
The heteroscorpionate N(2)S(2) donor ligand bis(3,5-tertbutylpyrazol-1-yl)dithioacetate (L) was prepared as a Li(+) trinuclear complex, which co-crystallizes with tetrahydrofuran (THF) solvent molecules: [Li(L)](3) x (2.25)THF. When [Li(L)](3) was reacted with AgBF(4) or [Cu(CH(3)CN)(4)]BF(4), the o...
|
PMID: 20604575
PDF is available here.
PDF is available here.
Abstract
We show that the ligand Hedgehog, the receptor Patched, and the transcription factor Gli are all expressed in striped patterns before the morphological appearance of segments in the annelid Platynereis dumerilii. Treatments with small molecules antagonistic to Hedgehog signaling disrupt segment form...
|
PMID: 20647470
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (285)29 2010
Abstract
We identified human phosphatidylethanolamine-binding protein 4 (hPEBP4) as a human-derived novel member of the phosphatidylethanolamine-binding protein family, which is involved in apoptosis resistance of tumor cells. Because of its preferential expression in estrogen-related cancers, we wondered wh...
|
PMID: 20460377
PDF is available here.
PDF is available here.
Abstract
We found that AMPK is strongly activated by tumor-like hypoxia and glucose deprivation, independently of the oxygen response system associated with HIF-1. We also observed high levels of AMPK activity in tumor cells in vivo, using different model tumors. These findings suggested the hypothesis that...
|
PMID: 20495370
PDF is available here.
PDF is available here.
Seminars in Hematology (47)3 2010
Abstract
Abstract
Our current findings uncover a novel mechanism by which AMPK protects against hypercholesterolemia-mediated endothelial dysfunction....
|
PMID: 20395595
PDF is available here.
PDF is available here.
Abstract
Celecoxib Transdermal patches were prepared by using different polymers such as hydroxyl-propylmethylcellulose (HPMC), methylcellulose (MC), Polyvinylpyrolidone (PVP). The in-vitro release of the drug from the formulations were studied using commercial semi permeable membrane. The prepared formulati...
|
PMID: 20566440
PDF is available here.
PDF is available here.