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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.
Enzyme Inhibitors (16):
- Folic Acid Antagonists
- Nucleic Acid Synthesis Inhibitors
- Cyclooxygenase Inhibitors
- Protein Synthesis Inhibitors
- Phosphodiesterase Inhibitors
- Monoamine Oxidase Inhibitors
- Lipoxygenase Inhibitors
- Protein Kinase Inhibitors
- Integrase Inhibitors
- Hydroxymethylglutaryl-CoA Reductase Inhibitors
- Proton Pump Inhibitors
- Cholinesterase Inhibitors
- Carbonic Anhydrase Inhibitors
- Uncoupling Agents
- Protease Inhibitors
- Aromatase Inhibitors
Recent article
Enzyme Inhibitors
Abstract
We reported that vitamin K₃ (menadione, 2-methyl-1,4-naphthoquinone) (compound 2) inhibits the activity of human mitochondrial DNA polymerase γ (pol γ). In this study, we investigated the inhibitory effects (IEs) of vitamin K3 and its derivatives, such as 1,4-naphthoquinone (compound 1) and 1,2-...
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PMID: 21837358
PDF is available here.
PDF is available here.
| < More recent | Older article > |
New England Journal of Medicine (365)14 2011
Abstract
We concluded a randomized trial involving 1088 patients with multiple sclerosis, 18 to 55 years of age, with a score of 0 to 5.5 on the Expanded Disability Status Scale and at least one relapse in the previous year or at least two relapses in the previous 2 years. Patients were randomly assigned (in...
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PMID: 21991951
PDF is available here.
PDF is available here.
New England Journal of Medicine (365)12 2011
Abstract
New England Journal of Medicine (365)12 2011
Abstract
A total of 432 patients underwent randomization to receive one of four doses of BIBF 1120 (50 mg once a day, 50 mg twice a day, 100 mg twice a day, or 150 mg twice a day) or placebo. In the group receiving 150 mg of BIBF 1120 twice a day, FVC declined by 0.06 liters per year, as compared with 0.19 l...
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PMID: 21992121
PDF is available here.
PDF is available here.
Circulation (124)10 2011
Abstract
We report that rat cardiac allograft ischemia/reperfusion injury resulted in profound microvascular dysfunction that was prevented by donor treatment with peroral single-dose simvastatin, a 3-hydroxy-3-methylglutaryl coenzyme A reductase and Rho GTPase inhibitor, 2 hours before graft procurement. Du...
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PMID: 21844074
PDF is available here.
PDF is available here.
Abstract
We show that two PARP1 inhibitors, PJ-34 and 3-AB, attenuate AKT phosphorylation at serine 473 (S473) independent of DNA repair impairment. These inhibitors decrease the AKT-associated phosphorylation of FOXO3A, enhance the nuclear retention of FOXO3A, and activate its transcriptional activity. We f...
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PMID: 21821012
PDF is available here.
PDF is available here.
Abstract
We present a data mining approach that enables the identification of alternative analog series with different core structures, corresponding substitution patterns, and comparable potency progression. Scaffolds can be exchanged between these series and new analogs suggested that incorporate preferred...
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PMID: 21774471
PDF is available here.
PDF is available here.
Abstract
The aim of this study was to evaluate the role of nitric oxide (NO) in the mechanisms of arterial distensibility and intravascular pressure stability in normotensive and spontaneously hypertensive rats. The experiments were performed on the anesthetized male Wistar, Wistar-Kyoto (WKY...
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PMID: 21961305
PDF is available here.
PDF is available here.
Abstract
We investigated the effects of Tan IIA on cardiac hypertrophy and fibrosis in two-kidney, two-clip (2K2C) hypertensive rats and by which, if any, mechanisms. Administration of 2K2C hypertensive rats with Tan IIA attenuated cardiac dysfunction and fibrosis. However Tan IIA treatment had no effects on...
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PMID: 21812327
PDF is available here.
PDF is available here.
Biochimica et Biophysica Acta (1807)11 2011
Abstract
Cytochrome bd is a respiratory quinol:O(2) oxidoreductase found in many prokaryotes, including a number of pathogens. The main bioenergetic function of the enzyme is the production of a proton motive force by the vectorial charge transfer of protons. The sequences of cytochromes bd are not homologous...
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PMID: 21756872
PDF is available here.
PDF is available here.
Seminars in Oncology (38) 2011
Abstract
Tumor resistance remains a major clinical challenge. Numerous pathways are under investigation to determine how best to target therapies to specific mutations in tumor biology and circumvent resistance. Agents in development include inhibitors of the poly(adenosine diphosphate [ADP]-...
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PMID: 21600381
PDF is available here.
PDF is available here.
Abstract
The cancer preventive activities of tea (Camellia sinensis, Theaceae) have been demonstrated in animal models for cancers at different organ sites and suggested by some epidemiological studies. Many mechanisms for cancer prevention have been proposed based on studies in cell lines, w...
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PMID: 21538856
PDF is available here.
PDF is available here.
Abstract
The effect of costunolide on the function of osteoblastic MC3T3-E1 cells was studied. Costunolide significantly increased the growth of MC3T3-E1 cells and caused a significant elevation of alkaline phosphatase (ALP) activity, collagen content, and mineralization in the cells (P<0.05)...
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PMID: 21296696
PDF is available here.
PDF is available here.
Revue medicale suisse (7)296 2011
Abstract
We will cover the results obtained with targeted therapies such as "tyrosin kinase inhibitors" (TKI), as well as those obtained with a monoclonal antibody directed against the CTLA-4 receptor of lymphocytes....
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PMID: 21721201
PDF is available here.
PDF is available here.
Revue medicale suisse (7)296 2011
Abstract
PARP inhibitors are novel drugs under development in oncology, particularly against breast and ovarian cancer. They act on the DNA repair mechanisms in synergy with the loss of BRCA function of the tumor cells, thereby inducing a genetic instability that leads to cell death. The clin...
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PMID: 21721203
PDF is available here.
PDF is available here.
Cancer Cell (19)5 2011
Abstract
We investigate the mechanisms by which ETS fusions mediate their effects, and find that the product of the predominant ETS gene fusion, TMPRSS2:ERG, interacts in a DNA-independent manner with the enzyme poly (ADP-ribose) polymerase 1 (PARP1) and the catalytic subunit of DNA protein kinase (DNA-PKcs)...
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PMID: 21575865
PDF is available here.
PDF is available here.
Xenobiotica (41)5 2011
Abstract
We focus on two sphingolipid signaling molecules, sphingosine-1-phosphate (S1P) and ceramide, as they are involved in cell fate decisions (survival vs. apoptosis) and in a wide range of pathophysiological processes. For S1P, we will discuss sphingosine kinases and S1P lyase as the enzymes which are...
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PMID: 18751924
PDF is available here.
PDF is available here.
Xenobiotica (41)5 2011
Abstract
We recently showed that isolated replication complexes are able to synthesize two species of nascent viral RNA, one double stranded and the other single stranded. NS5B nucleoside inhibitors block synthesis of both species, whereas nonnucleoside inhibitors inhibit mostly single- tranded RNA synthesis...
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PMID: 19009261
PDF is available here.
PDF is available here.
Medicinal Chemistry (7)3 2011
Abstract
We have performed QSAR, pharmacophore mapping and molecular docking studies of cycloguanil derivatives as Plasmodium falciparum dihydrofolate reductase thymidylate synthase (PfDHFR-TS) inhibitors to explore essential features required for the antimalarial activity and important interaction patterns...
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PMID: 21486210
PDF is available here.
PDF is available here.
Journal of Immunotherapy (34)4 2011
Modulation of the poliovirus receptor expression in malignant lymphocytes by epigenetic alterations.
Abstract
We have studied the mechanism of this defective expression of PVR. We demonstrated that the characterization of NK-insensitive cell lines was of low expression of PVR in both mRNA and surface levels, and that PVR of RAJI cells able to resist NK cells has hypermethylated promoter-associated CpG islan...
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PMID: 21499126
PDF is available here.
PDF is available here.
Nature Immunology (12)5 2011
Abstract
We show that the saturated fatty acid palmitate, but not unsaturated oleate, induces the activation of the NLRP3-ASC inflammasome, causing caspase-1, IL-1β and IL-18 production. This pathway involves mitochondrial reactive oxygen species and the AMP-activated protein kinase and unc-51-like kinase-1...
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PMID: 21478880
PDF is available here.
PDF is available here.
Abstract
We developed a new method utilizing an epoxide of arachidonic acid (14(15)-EpETrE) as substrate. Incubation samples were directly injected without purification into an online solid phase extraction (SPE) liquid chromatography electrospray ionization tandem mass spectrometry (LC-ESI-MS-MS) setup allo...
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PMID: 21479549
PDF is available here.
PDF is available here.
Abstract
We show in hippocampal CA1 pyramidal neurons that the NR2B to NR2A switch driven acutely by activity requires activation of NMDARs and mGluR5, involves PLC, Ca(2+) release from IP(3)R-dependent stores, and PKC activity. In mGluR5 knockout mice the developmental NR2B-NR2A switch in CA1 is deficient....
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PMID: 21521618
PDF is available here.
PDF is available here.
Circulation (123)14 2011
Abstract
Circulation (123)14 2011
Abstract
Abstract
Hydrogen sulfide (H2S), the colorless gas with the smell of rotten eggs, has been regarded as a novel gaseous signaling molecule. Although H2S has been proved been involved into the cardiovascular functions, the cardiovascular functions of H2S within the nucleus tractus solitarii (NT...
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PMID: 21612157
PDF is available here.
PDF is available here.
Abstract
We have previously shown that the foreign body reaction (FBR) against crosslinked collagen type I (Col-I) differs between subcutaneous and epicardial implantation sites; Col-I was quickly degraded epicardially, whereas degradation was attenuated subcutaneously. The current study set out to dissect t...
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PMID: 20661871
PDF is available here.
PDF is available here.
Abstract
We will summarize the PI3K signaling network and discuss current strategies for pathway inhibition. We will also explore the importance and emerging relevance of Akt-independent PI3K signaling pathways and discuss attempts being made to harness these pathways by inhibiting the binding of a product o...
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PMID: 21526896
PDF is available here.
PDF is available here.
Abstract
We will summarize the PI3K signaling network and discuss current strategies for pathway inhibition. We will also explore the importance and emerging relevance of Akt-independent PI3K signaling pathways and discuss attempts being made to harness these pathways by inhibiting the binding of a product o...
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PMID: 21526896
PDF is available here.
PDF is available here.
Abstract
We investigated the effects of two different inhibitors of MAPK signaling in proliferative and invasive melanoma cell cultures with various mutations in the MAPK pathway. Proliferative melanoma cells were more susceptible to pathway inhibition than invasive phenotype cells, irrespective of BRAF muta...
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PMID: 21176117
PDF is available here.
PDF is available here.
Abstract
We have conducted studies on the drug resistance through docking and binding analysis supported by time-scale (∼ 1000 ps) and unrestrained all-atom molecular dynamics simulations of wild and mutant MtBKatG. The study showed conformational changes of binding residues. Mutant (S315T) showed high doc...
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PMID: 20593210
PDF is available here.
PDF is available here.
Abstract
We have established an RNA interference (RNAi) screen to identify genes whose depletion selectively inhibits the growth of cells lacking BRCA2, and then studied the effects of the genetic depletion or pharmacologic inhibition of 1 candidate, the checkpoint kinase 1 (CHK1), in the context of pancreat...
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PMID: 21289082
PDF is available here.
PDF is available here.
Abstract
We investigated the mechanism that enables paullones to selectively inhibit GSK-3 rather than cyclin-dependent kinase 5 (CDK5) using sequence alignment, molecular dynamics simulations, free-energy calculations and free-energy decomposition analysis. The results indicate that the interaction between...
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PMID: 20559856
PDF is available here.
PDF is available here.
Abstract
We investigated the mechanism that enables paullones to selectively inhibit GSK-3 rather than cyclin-dependent kinase 5 (CDK5) using sequence alignment, molecular dynamics simulations, free-energy calculations and free-energy decomposition analysis. The results indicate that the interaction between...
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PMID: 20559856
PDF is available here.
PDF is available here.
Molecular Therapy (19)3 2011
Abstract
A major hurdle for harnessing small interfering RNA (siRNA) for therapeutic application is an effective and safe delivery of siRNA to target tissues and cells via systemic administration. While lipid nanoparticles (LNPs) composed of a cationic lipid, poly-(ethylene glycol) lipid and...
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PMID: 21179008
PDF is available here.
PDF is available here.
Abstract
In patients with active rheumatoid arthritis despite therapy with DMARDS, treatment with a spleen tyrosine kinase inhibitor has achieved similar response rates to those achieved in clinical trials of other drugs, including biologic agents. Where might these agents fit in the current...
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PMID: 21304505
PDF is available here.
PDF is available here.
Abstract
We review recent advances in validation of SCF E3 ubiquitin ligase complex as an attractive anti-cancer target and discuss how MLN4924, a small molecule inhibitor of NEDD8-activating enzyme, can be developed as a novel class of anticancer agents by inhibiting SCF E3 ligase complex via removal of cul...
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PMID: 21247385
PDF is available here.
PDF is available here.
Abstract
Anemia is an important complication of inflammatory bowel disease (IBD). Recent data suggest that hepcidin is a major mediator of anemia with a central role in iron homeostasis and metabolism. The aim of this study was to evaluate the serum levels of hepcidin and its prohormone, proh...
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PMID: 21285884
PDF is available here.
PDF is available here.
Cancer Cell (19)2 2011
Abstract
We report that the Notch ligand Jagged1 is a clinically and functionally important mediator of bone metastasis by activating the Notch pathway in bone cells. Jagged1 promotes tumor growth by stimulating IL-6 release from osteoblasts and directly activates osteoclast differentiation. Furthermore, Jag...
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PMID: 21295524
PDF is available here.
PDF is available here.
Cancer Cell (19)2 2011
Abstract
We report that the Notch ligand Jagged1 is a clinically and functionally important mediator of bone metastasis by activating the Notch pathway in bone cells. Jagged1 promotes tumor growth by stimulating IL-6 release from osteoblasts and directly activates osteoclast differentiation. Furthermore, Jag...
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PMID: 21295524
PDF is available here.
PDF is available here.
Journal of Proteomics (74)2 2011
Abstract
We report here a proteomic analysis of bean seeds by two-dimensional electrophoresis (2-DE). Three different protein extraction methods (TCA-acetone, phenol and the commercial clean-up kit) were used taking into account that the extractome can have a determinant impact on the level of quality of dow...
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PMID: 20971221
PDF is available here.
PDF is available here.
Journal of Physiology (589)Pt 3 2011
Abstract
Arthritis & Rheumatism (63)2 2011
Abstract
Our findings indicate that there were no differences in the primary end point between the R788 and placebo groups. Differences were observed between the R788 and placebo groups in secondary end points, particularly in those patients who entered the study with an elevated CRP level.
C...
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PMID: 21279990
PDF is available here.
PDF is available here.
Abstract
Abstract
We previously found that some catechins, such as epigallocatechin-3-O-gallate (EGCG), inhibit the activities of eukaryotic DNA polymerases (pols) (Y. Mizushina et al.: Structural analysis of catechin derivatives as mammalian DNA polymerase inhibitors. Biochem Biophys Res Commun 333, 101-109 (2005))....
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PMID: 21622140
PDF is available here.
PDF is available here.
Science Signaling (4)174 2011
Abstract
Adenosine 5'-diphosphate (ADP)-ribosylation is a protein posttranslational modification that is catalyzed by ADP-ribosyltransferases (ARTs), using nicotinamide adenine dinucleotide (NAD(+)) as a substrate. Mono-ribosylation can be extended into polymers of ADP-ribose (PAR). Poly(ADP-...
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PMID: 21610250
PDF is available here.
PDF is available here.
Abstract
This review summarizes current knowledge of adenosine analogues and conjugates with promising therapeutic properties. Adenosine is a signaling molecule that triggers numerous physiological responses. It acts through the adenosine receptors (ARs), belonging to the family of G-protein-...
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PMID: 21857072
PDF is available here.
PDF is available here.
Abstract
Organophosphate (OP) nerve agents such as sarin, soman, tabun, and O-ethyl S-[2-(diisopropylamino) ethyl] methylphosphonothioate (VX) do not react solely with acetylcholinesterase (AChE). Evidence suggests that cholinergic-independent pathways over a wide range are also targeted, inc...
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PMID: 21120745
PDF is available here.
PDF is available here.
Abstract
We reviewed preclinical data and clinical development of MDM2 (murine double minute 2), ALK (anaplastic lymphoma kinase) and PARP (poly [ADP-ribose] polymerase) inhibitors. MDM2 binds to p53, and promotes degradation of p53 through ubiquitin-proteasome degradation. JNJ-26854165 and RO5045337 are 2 s...
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PMID: 21504625
PDF is available here.
PDF is available here.
Vascular Pharmacology (54)3-6 2011
Abstract
We investigated the potential of Jak2 inhibition to counteract Nox-dependent O(2)(•-) formation in atherogenesis in hypercholesterolemic apolipoprotein E-deficient (ApoE(-/-)) mice. Male ApoE(-/-) mice fed a high-fat, cholesterol-rich diet were treated for 5 weeks with either vehicle or tyrphostin...
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PMID: 21457788
PDF is available here.
PDF is available here.
Abstract
We tested gene expression of PI3K, AKT1, JUN, CASP3 and DDIT3 in K562, BaF3P210(BCR-ABL) and BaF3 P210(BCR-ABLT315I) cell line treated for 6- and 12- hours with NPB001-05 and imatinib. The data indicates that NPB001-05 mediated cell death in K562 affects the function of ER stress. NPB001-05 shows an...
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PMID: 21622141
PDF is available here.
PDF is available here.
Abstract
We exploited the PI3K/Akt dependent cytoprotective effect of Tat-expressing CHME5 cells. We screened a collection of compounds known to modulate inflammation, and identified three novel compounds: Lancemaside A, Compound K and Arctigenin that abolished the cytoprotective phenotype of Tat-expressing...
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PMID: 21765914
PDF is available here.
PDF is available here.
Neonatology (99)2 2011
Abstract
We studied the effects of lipopolysaccharide (LPS) on expression and function of NF-κB and p38 MAPK in whole neonatal cord and adult blood.
Th1/Th2 cytokine concentrations and phosphorylation of NF-κB and p38 MAPK were determined by flow-cytometric analysis.
Tumor n...
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PMID: 20798552
PDF is available here.
PDF is available here.
Abstract
T cells are known for their contribution to the inflammatory element of atherosclerosis. Recently, it has been demonstrated that the Th17 derived cytokine IL-17 is involved in the pro-inflammatory response of vascular smooth muscle cells (VSMC). The aim of the present study was to examine whether re...
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PMID: 20606471
PDF is available here.
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.
PDF is available here.
Oxygen-dependent vasomotor responses are conducted upstream in the mouse cremaster microcirculation.
Abstract
We tested whether hypoxic vasodilation and hyperoxic vasoconstriction in arterioles in striated muscle are being propagated upstream, and whether the endothelium and smooth muscle cell layers are necessary components in the signaling pathway.
The study was performed in mouse cremaster muscle superfu...
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PMID: 20639650
PDF is available here.
PDF is available here.
Abstract
Multiproperty lead optimization that satisfies multiple biological endpoints remains a challenge in the pursuit of viable drug candidates. Optimization of a given lead compound to one having a desired set of molecular attributes often involves a lengthy iterative process that utilizes existing infor...
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PMID: 20981525
PDF is available here.
PDF is available here.
Abstract
Mammalian paraoxonases (PONs) are a unique, highly conserved family of calcium-dependent esterases consisting of PON1, PON2, and PON3. The PONs can hydrolyze the lactone ring of a range of N-acyl-L: -homoserine lactone (AHL) quorum sensing signaling molecules, rendering them inactive. This chapter d...
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PMID: 21031320
PDF is available here.
PDF is available here.
Biochimica et Biophysica Acta (1811)1 2011
Abstract
We observed lactonase activity in serum from Pon1-/- mice. However, 6-12 carbon fatty acid γ- and δ-lactones were not hydrolyzed in serum from Pon1-/- mice. Serum from both wild-type and Pon1-/- mice contained a lactonase activity towards 5-HETEL and 3-oxo-dodecanoyl-homoserine lactone that was re...
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PMID: 21044894
PDF is available here.
PDF is available here.
Abstract
We have developed a rapid visual in vitro assay to detect toxicity mediated by individual WA particles in cultured L6-C11 rat muscle cells. Using a variety of techniques (histology, comet assay, caspase-3 activity, oxidation of 2'7'-dichlorofluorescin to measure the production of reactive oxygen spe...
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PMID: 20934443
PDF is available here.
PDF is available here.