John C Breitner,
Laura D Baker,
Thomas J Montine,
Curtis L Meinert,
Constantine G Lyketsos,
Karen H Ashe,
Jason Brandt,
Suzanne Craft,
Denis E Evans,
Robert C Green,
M Saleem Ismail,
Barbara K Martin,
Michael J Mullan,
Marwan Sabbagh,
Pierre N Tariot and
ADAPT Research Group
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...
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PMID: 21784351
PDF is available here.
Nasser K Altorki,
Paul Christos,
Jeff L Port,
Paul C Lee,
Farooq Mirza,
Cathy Spinelli,
Roger Keresztes,
Debra Beneck,
Subroto Paul,
Brendon M Stiles,
Yuwei Zhang and
David S Schrump
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...
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PMID: 21532508
PDF is available here.
Abstract
These results indicate a critical role for TLR4 in impairing renal function during ovine endotoxemia that is independent of changes in central hemodynamics....
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PMID: 21394006
PDF is available here.
Abstract
These results indicate a critical role for TLR4 in impairing renal function during ovine endotoxemia that is independent of changes in central hemodynamics....
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PMID: 21394006
PDF is available here.
Abstract
Our primary goal was to determine whether OPG provided independent prognostic information in patients with chronic HF, and to examine its potential interactions with statin therapy.
OPG as a risk factor for the primary end point (cardiovascular death, nonfatal myocardial infarction,...
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PMID: 21216833
PDF is available here.
Abstract
The aim of this study is to examine the effect and mechanism of a selective cyclooxygenase-2 (COX-2) inhibitor NS-398 on inducing apoptosis of esophageal cancer cells. After the treatment with NS-398 on esophageal carcinoma EC9706 cell, MTT assay was used to observe the inhibition of...
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PMID: 21329005
PDF is available here.
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...
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PMID: 21079613
PDF is available here.
Abstract
The thermodynamic aspects of solubility process of sulfonamides with the general structures C(6)H(5)-SO(2)NH-C(6)H(4)-R (R=4-NO(2); 4-Cl) and 4-NH(2)-C(6)H(4)-SO(2)NH-C(6)H(4)-R (R=4-NO(2); 4-CN; 4-Cl; 4-OMe; 4-C(2)H(5)) in water, phosphate buffer with pH 7.4 and n-octanol (as phases modeling variou...
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PMID: 20801596
PDF is available here.
Abstract
Structure-based library design employs both structure-based drug design (SBDD) and combinatorial library design. Combinatorial library design concepts have evolved over the past decade, and this chapter covers several novel aspects of structure-based library design together with successful case stud...
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PMID: 20981524
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....
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PMID: 21220497
PDF is available here.
M R MR Preusch,
A A Vanakaris,
F F Bea,
N N Ieronimakis,
T T Shimizu,
M M Konstandin,
S S Morris-Rosenfeld,
C C Albrecht,
A A Kranzhöfer,
H A HA Katus,
E E Blessing and
R R Kranzhöfer
Abstract
We investigated the effect of the HMG-CoA reductase inhibitor rosuvastatin on MMP-9 expression and neointima formation.
14-week old male Sprague Dawley rats underwent balloon injury of the common carotid artery. Half of the animals received rosuvastatin (20 mg/kg body weight/day) via oral gavage, be...
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PMID: 21159570
PDF is available here.
Abstract
Tamsulosin, an alpha1 adrenoceptor blocking agent, exhibits selectivity for alpha1 receptors in human prostate. Blockade of these adrenoceptors can cause smooth muscles in the bladder neck and prostate to relax, resulting in an improvement in urine flow rate and a reduction in symptoms of benign pro...
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PMID: 21084043
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...
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PMID: 20937254
PDF is available here.
Abstract
We have previously shown that a high cholesterol (HC) diet results in increases in microglia load and levels of the pro-inflammatory cytokine interleukin-6 (IL-6) in the brains of wild type (WT) and apolipoprotein E knockout (ApoE-/-) mice. In the present investigation, we analyzed whether treatment...
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PMID: 20946880
PDF is available here.
Abstract
Despite clear guideline recommendations, there is a growing body of evidence that there is suboptimal use of lipid-lowering treatment in Canadians.
To assess the prevalence and types of persistent lipid abnormalities in Canadian patients receiving statin therapy.
The present cross-sectional study re...
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PMID: 21076724
PDF is available here.
Abstract
Our aim is to discuss recent developments on this rapidly evolving topic.
Sunitinib represents front-line standard treatment for the good- and intermediate prognosis groups of patients with clear cell renal carcinoma. Bevacizumab/interferon and pazopanib have also been FDA-approved as first-line age...
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PMID: 21129605
PDF is available here.
Abstract
We sought to evaluate current practice patterns of MET among urologists, emergency medicine physicians, other primary care providers, and frontline military care providers.
Web-based, self-developed survey to assess the current practice patterns of providers for the initial management of uncomplicat...
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PMID: 21121500
PDF is available here.
Abstract
We previously demonstrated that in an infant rat model of pneumococcal meningitis, there is activation of the kynurenine (KYN) pathway in the hippocampus, and that there was a positive correlation between the concentration of 3-hydroxykynurenine and the extent of hippocampal apoptosis. To clarify th...
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PMID: 20940631
PDF is available here.
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...
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PMID: 20654703
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...
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PMID: 20697803
PDF is available here.
Abstract
The effects of cyclooxygenase (COX) inhibition on fracture healing are insufficiently documented, and the aim of this study was to evaluate the effects of nonspecific and specific COX-2 inhibition in the early phase of fracture healing.
Thirty rats were randomized in three groups. A diaphyseal fract...
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PMID: 20874480
PDF is available here.
Abstract
The aim of this study was to describe the long-term outcomes in idiopathic pulmonary arterial hypertension (IPAH) treated with first-line bosentan or intravenous (IV) epoprostenol, and additional therapy as needed.
In a single-center, retrospective, longitudinal cohort, data on right heart catheteri...
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PMID: 20580264
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....
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PMID: 20121624
PDF is available here.
Abstract
We assayed the content of endotoxin in the commercial alpha-LA. We found to our surprise that endotoxin was there and that alpha-LA-induced NO and PGE(2) production could be suppressed by polymyxin B, a specific inhibitor of endotoxin. Thus, the pro-inflammatory effects of commercial alpha-LA might...
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PMID: 20600530
PDF is available here.
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....
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PMID: 21036716
PDF is available here.
Abstract
A 54-year-old woman with a 20-year history of Raynaud phenomenon was admitted to our hospital complaining of progressive dyspnea on exertion since 5 years previously. Interstitial lung disease was diagnosed, accompanied by pulmonary arterial hypertension (PAH) associated with systemic sclerosis. Aft...
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PMID: 21066870
PDF is available here.
Abstract
Dalcetrapib targets cholesteryl ester transfer protein and increases high-density lipoprotein cholesterol (HDL-C) levels. It is in clinical development for the prevention of cardiovascular events and will likely be used in combination with standard of care, including statins. Three crossover studies...
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PMID: 20489031
PDF is available here.
Abstract
We examined the effects of nominally selective inhibitors of PI3K (wortmannin, PI103, GDC-0941), SGK1 (GSK650394A) and PKB (Akti-1/2) on Na(+) transport in hormone-deprived and insulin-stimulated cortical collecting duct (mpkCCD) cells, while PI3K, SGK1 and PKB activities were assayed by monitoring...
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PMID: 20880397
PDF is available here.
Abstract
Asparaginases are a cornerstone of treatment protocols for acute lymphoblastic leukemia (ALL) and are used for remission induction and intensification treatment in all pediatric regimens and in the majority of adult treatment protocols. Extensive clinical data have shown that intensive asparaginase t...
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PMID: 20824725
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...
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PMID: 20813338
PDF is available here.
Abstract
Sulfonamide bearing compounds possess many types of biological activities and have recently been reported to show substantial antitumor activity in vitro and/or in vivo. There are a variety of mechanisms for the anticancer activity, and the most prominent mechanism is the inhibition of carbonic anhy...
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PMID: 20684857
PDF is available here.
Abstract
We intend to update the data of various clinical features and management of sarcoidosis in the aged.
Subclinical or inapparent systemic involvement of sarcoidosis was found at autopsy in elderly patients who died from sarcoidosis, complication of malignancy, or cerebrovascular accidents. Sarcoidosis...
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PMID: 20473168
PDF is available here.
Abstract
These results indicate that enhancement of cholesterol efflux activity may have the potential to reduce bioprosthetic and native valve degeneration....
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PMID: 21053746
PDF is available here.
Abstract
We and other groups reported that liver X receptor (LXR) agonists T0901317, 22(R)-hydroxycholesterol, and 24(S)-hydroxycholesterol suppressed the proliferation of prostate and breast cancer cells. In this study, we report that T0901317 and 22(R)-hydroxycholesterol treatment inhibited the proliferati...
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PMID: 20944148
PDF is available here.
Abstract
A review was conducted to examine the published works that studied the prevalence of Pneumocystis jirovecii dihydropteroate synthase (DHPS) mutations in patients with P. jirovecii pneumonia (PcP), in develop and developing countries, and that focused the problem of the possible association of these...
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PMID: 21073145
PDF is available here.
Abstract
I and II clinical trials conducted to date have demonstrated that macitentan increases plasma levels of ET-1, displays dose-dependent pharmacokinetics, and was well tolerated in healthy volunteers and patients. At the time of publication, a phase II trial in patients with IPF and a phase III trial i...
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PMID: 20730702
PDF is available here.
Abstract
We report the discovery of a small molecule that binds to pirin. We determined how the small molecule bound to pirin by solving the cocrystal structure. Either knockdown of pirin or treatment with the small molecule inhibited melanoma cell migration. Thus, inhibition of pirin by the small molecule h...
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PMID: 20711196
PDF is available here.
Abstract
A prospective randomized controlled study was performed to compare the clinical effects of naftopidil and tamsulosin. Men complaining of lower urinary tract symptoms due to benign prostatic hyperplasia were randomized into two groups : one receiving 50mg naftopidil once daily (Naf group, n=36 patien...
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PMID: 20940522
PDF is available here.
Abstract
Droperidol has more detrimental effects on cardiac repolarization of LQT1-like than of LQT2-like myocytes suggesting subtype-specific cardiotoxic effects in patients with LQT syndrome. The subtype specificity of droperidol seems to be caused by a complex interaction of droperidol with several differ...
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PMID: 20601449
PDF is available here.
Abstract
We used a series of molecules known to inactivate various elements of the pathway. W-7 prevents CaM from interacting with other molecules. Neomycin isolates PIP(2) from PLC. U-73122 directly inactivates PLC. 2-APB blocks IP(3) receptors which would otherwise cause release of Ca(2+). Verapamil and Cd...
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PMID: 20416320
PDF is available here.
Abstract
As recently discovered, matriptase-2, a type II transmembrane serine protease, plays a crucial role in body iron homeostasis by down-regulating hepcidin expression, which results in increased iron levels. Thus, matriptase-2 represents a novel target for the development of enzyme inhibitors potential...
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PMID: 20684597
PDF is available here.
Abstract
Three COX-2-specific non-steroidal anti-inflammatory drugs (NSAIDs), etoricoxib, parecoxib, and nimesulide are widely prescribed against inflammatory conditions. However, their long term administration leads to severe conditions of cardiovascular complications and gastric ulceration. In order to min...
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PMID: 20515646
PDF is available here.
Abstract
We investigated the antitumor activity of JTP-70902, a novel specific MEK inhibitor, against human fibrosarcoma cells in which the ERK pathway is constitutively activated. JTP-70902 was synthesized at Japan Tabacco. Human fibrosarcoma HT1080 cells were cultured. JTP-70902 was added at various concen...
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PMID: 20596617
PDF is available here.
Abstract
We examined the effect of the selective COX-1 inhibitor, FR122047 and the selective COX-2 inhibitor, SC791 on cell growth and apoptosis in human breast cancer MCF-7 cells which exhibited a high basal level of COX-1 expression. Compared to SC791, FR122047 treatment led to a distinct suppression of ce...
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PMID: 20596620
PDF is available here.
Abstract
We show that CaMKII activation and postsynaptic translocation induce the synaptic trapping of AMPARs diffusing in the membrane. AMPAR immobilization requires both phosphorylation of the auxiliary subunit Stargazin and its binding to PDZ domain scaffolds. It does not depend on the PDZ binding domain...
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PMID: 20670832
PDF is available here.
Abstract
I (hCA I), but which is near the substrate binding pocket of the enzyme. This change led to a steady increase of 16% of the catalytic activity of the mutant hCA I over the wild type enzyme, which is a gain of 50% catalytic efficiency if one compares hCA I and hCA II as catalysts for CO(2) hydration....
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PMID: 20624682
PDF is available here.
Abstract
The present study was planned to investigate the antioxidant, antinociceptive, and anti-inflammatory activities of atorvastatin and rosuvastatin (1, 3 and 10 mg/kg, p.o.) in various animal models. The antinociceptive effect was assessed by chemically- (formalin, acetic acid) and thermally- (hot plat...
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PMID: 20532641
PDF is available here.
Abstract
We studied these aspects in the Measuring Effects on intima media Thickness: an Evaluation Of Rosuvastatin (METEOR) study, a randomized placebo-controlled trial amongst 984 low-risk subjects.
METEOR is a randomized placebo-controlled trial that evaluated the effect of 40 mg of rosuva...
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PMID: 20412373
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...
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PMID: 20718170
PDF is available here.