discovery of selective and potent inhibitors of palmitoylation
Báo cáo Y học: Selection of effective antisense oligodeoxynucleotides with a green fluorescent protein-based assay Discovery of selective and potent inhibitors of glutathione S-transferase Mu expression doc
... set of 15 PS-ODNs These ODNs selectively inhibit the expression of GSTM1 and/ or GSTM2 and can be used to study the influence of reduced GSTM expression on the detoxification of xenobiotics and ... effectiveness of a set of antisense PS-ODNs directed against the glutathione S-transferase Mu1 (GSTM1) and Mu2 (GSTM2) isoforms of the rat GSTs play an important role in the detoxification of DNA- and/ or ... by summation of the molecular weights of EGFP (25 kDa) and GSTM (27 kDa) Colocalization of ODN and pEGFP For proper evaluation of antisense effects, it is important that the AS-ODNs and the EGFP-expressing...
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Báo cáo hóa học: " Hepatitis C virus NS2 and NS3/4A proteins are potent inhibitors of host cell cytokine/chemokine gene expression" potx
... and TBK1 [7-10,12], which leads to activation and nuclear translocation of NF-κB and IRF3 [13,14] In the nucleus IRF3, NF-κB and AP-1 (ATF-2/c-Jun) transcription factors activate type I IFN and ... design of the study, performed most of the experiments, analysed the results and drafted the manuscript MS participated in the design of the study and carried out some experiments SK, RL and JH ... preparation of cell lysates and measurement of luciferase activities (Fig 1) Sendai virus was used since it is able to activate NF-κB, IRF and MAP kinase pathways that regulate the expression of chemokine...
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Báo cáo y học: "The discovery of potential acetylcholinesterase inhibitors: A combination of pharmacophore modeling, virtual screening, and molecular docking studies" pptx
... ligands such as decamethonium [10] and donepezil [19] extend to the mouth of the gorge, the opening of the hydrophobic pocket Page of 13 The drug discovery process is both time-consuming and ... positives), and predicted 13 active compounds as inactive (false negatives) An enrichment factor of 38.61 and a GH score of 0.73 indicated the quality of the model and high efficiency of the screening ... as: Lu et al.: The discovery of potential acetylcholinesterase inhibitors: A combination of pharmacophore modeling, virtual screening, and molecular docking studies Journal of Biomedical Science...
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Báo cáo y học: ""Shock and kill" effects of class I-selective histone deacetylase inhibitors in combination with the glutathione synthesis inhibitor buthionine sulfoximine in cell line models for HIV-1 quiescence" doc
... (p50/p50 homodimers), AP-4, Sp1, YY1 and c-Myc [12-14] Identification of class/ isoform -selective HDACIs with increased potency and lower toxicity [3] and drugs able to potentiate their effects is believed ... between the results in the ACH2 and U1 cells (Figure 1) Only non-class selective and class I -selective HDACIs were significantly active (Figure 1), and potent class I -selective HDACIs enhanced HIV-1 ... replication in U1 and ACH-2 cells, and toxicity in uninfected JurPotencies Potencies of different HDACIs in terms of activation of HIV-1 replication in U1 and ACH-2 cells, and toxicity in uninfected...
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Development and application of a high throughput assay for discovery of starch hydrolase inhibitors
... in units of two or three, and the combined action of salivary and pancreatic amylase leads to the production of large amounts of maltose and maltotriose, and relatively small amounts of limit ... Determination of total phenolic content of grape seeds extracts - 120 7.3.2 Determination of the proanthocyanidin profiles of grape seeds extracts - 120 7.3.3 Determination of IC50 values of ... hydrolases Table Determination of the linear range of gelatinized starch Table Accuracy and precision of the high-throughput method Table IC50 and acarbose equivalence of inhibitors obtained by starch...
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Web Mining and Knowledge Discovery of Usage Patterns
... modeling of Web objects (products, service, pages etc) and subjects (users), categorization of objects and subjects, mapping between and across objects and/ or subjects, and determination of the set of ... semantics, and the support of navigation [2] J Borges and M Levene Data mining of user navigation patterns In Proceedings of the WEBKDD’99 Workshop on Web Usage Analysis and User Profiling, August ... Analysis process and makes use of the preprocessed content and structure information to automatically filter the results of the knowledge discovery algorithms for patterns that are potentially interesting...
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Tài liệu Ghost Wave - The Discovery of Cortes Bank and the Biggest Wave on Earth pptx
... twenty miles out and around the southern end of Catalina Island They would then cross another thirty-two miles of ocean to the southern flank of San Clemente Island, a naval base and artillery range ... up and scare Chief Brody and then slide back down in the water.” Sharp and Hulse triangulated using their homemade buoys and took a position just to the east of a spot of water that boiled and ... surfboard, and leapt over the gunwale, simultaneously and spectacularly spewing his breakfast into the deep blue sea The buoys stayed anchored, offering the surfers a point of reference and a measure of...
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Tài liệu Báo cáo khoa học: Biochemical characterization and inhibitor discovery of shikimate dehydrogenase from Helicobacter pylori docx
... properties of HpSDH and the effects of pH and temperature on HpSDH The results show that HpSDH has a kcat of 7.7 ± 0.9 s)1, Km of 0.148 ± 0.028 mm and kcat ⁄ Km of 5.2 · 104 m)1Æs)1 toward shikimate, and ... binding substrate and NADP cofactor The detailed structural information might expedite the discovery of novel SDH inhibitors and further of antimicrobial agents, though few SDH inhibitors have ... other hand, compounds 1, 4, and are noncompetitive inhibitors, and compounds and are competitive inhibitors with respect to NADP Table summarizes the IC50 values and kinetic inhibition data of compounds...
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Báo cáo khoa học: "Unsupervised Discovery of Generic Relationships Using Pattern Clusters and its Evaluation by Automatically Generated SAT Analogy Questions" pot
... restrictions), the degrees of supervision and required preprocessing, and evaluation method 2.1 Relationship Types There is a large body of related work that deals with discovery of basic relationship ... (Davidov and Rappoport, 2006; Widdows and Dorow, 2002) and meronymy (Berland and Charniak, 1999; Girju et al., 2006) Since named entities are very important in NLP, many studies define and discover ... modify the relative weight of core and unconfirmed patterns Corpora and Parameters In this section we describe our experimental setup, and discuss in detail the effect of each of the algorithms’ parameters...
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Báo cáo khoa học: "Efficient Unsupervised Discovery of Word Categories Using Symmetric Patterns and High Frequency Words" ppt
... greater: Discovery of Patterns Our first step is the discovery of patterns that are useful for lexical category acquisition We use two main stages: discovery of pattern candidates, and identification of ... fragments ‘book and newspaper’, ‘newspaper and book’, ‘book and note’, ‘note and book’ and ‘note and newspaper’ In this case the three words are assigned to a category Note that a pair of nodes connected ... The two main approaches are pattern-based discovery and clustering of context feature vectors Many of the papers cited below aim at the construction of hyponym (is-a) hierarchies Note that they...
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Báo cáo khoa học: Polyphosphates from Mycobacterium bovis – potent inhibitors of class III adenylate cyclases pptx
... IC50 of 20 lm, and the cyclic trimetaphosphate an IC50 of mm; that is, these compounds were poor inhibitors (Table 2) In contrast, all IC50 concentrations of poly-Ps with a chain length of 16 ... M urea) of inhibitory fractions from (A) Note almost empty lanes 46 and 48, which are barely inhibitory Controls of linear polyPs with average chain lengths of 75 (14 lg), 45 (7 lg), and 25 (7 ... inhibition of combined fractions from the Superose fractionation in (A) 1096 C E B A B Fig 31P-NMR spectra of the concentrated fractions (50–64) of the Superose gel filtration and of commercial...
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Báo cáo sinh học: " Discovery of herpesviruses in multi-infected primates using locked nucleic acids (LNA) and a bigenic PCR approach" pdf
... (gB), and two thirds of the ORF UL54 (DPOL) (Figure 6B) The nucleotide and amino acid sequence differences of CgueCMV-1.1 and CgueCMV-1.2 were 0.6% and 0.5% (UL56), 20% and 8% (UL55) and 1% and ... analysis of herpesvirus-positive blood and tissue samples of primates Samples of two chimpanzees ("Noah" and "Leo"; Pan troglodytes verus), which lived in the Taï National Park of Côte d'Ivoire and ... LCV-1) and 93% (LCV-3 versus LCV-2) were obtained Discovery of cytomegaloviruses in LCV-positive samples of a black -and- white colobus Blood, spleen, brain, kidney, bone marrow, stomach and mucosa of...
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Báo cáo sinh học: "Of mice and men: phylogenetic footprinting aids the discovery of regulatory elements." doc
... human genome and use Journal of Biology 2003, 2:11 11.4 Journal of Biology 2003, Volume 2, Issue 2, Article 11 Zhang and Gerstein them as a blueprint for understanding the mysteries of gene regulation ... TFBSs Lenhard and colleagues [6] collected TFBSs from both in vivo and in vitro assays and used an improved motif discovery algorithm, ANN-Spec [21], to construct over 100 distinct and high-quality ... required conservation (cut-off), and the length of sequence to search (window size) It is becoming evident that comparative genome analysis is very powerful and will be of use not only for genome...
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Báo cáo y học: " Adding 5-hydroxytryptamine receptor type 3 antagonists may reduce drug-induced nausea in poor insight obsessive-compulsive patients taking off-label doses of selective serotonin reuptake inhibitors: a 52-week follow-up case report" potx
... Indeed, his lack of insight of illness probably led to complete withdrawal of medication during that period of time and worsening of illness with progressive reduction of insight When he eventually ... Diagnostic and Statistical Manual of Mental Disorders, fourth edition (DSM-IV) criteria assessed by administration of the Structured Clinical Interview of Axis-I and Axis-II Disorder (SCID-I and SCID-II) ... impact of side effects in the course of therapy, highlighting a ‘distressing’ level of nausea The fluoxetine dose was reduced to 60 mg/day, adding 30 mg/day of mirtazapine and 10 mg/day of olanzapine...
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Báo cáo y học: "Local expression of matrix metalloproteinases, cathepsins, and their inhibitors during the development of murine antigen-induced arthritis" pps
... volume of 25 µl, consisting of 2.5 µl of 10 × PCR buffer, 2.0–2.5 µl of MgCl2 (25 mM), 0.5 µl of dNTPs (10 mM each; Promega), 0.5 µl of Hot Star Taq (5 U/µl), 0.5 µl of primer mix (20 µM each) and ... proteinases and deregulation of the balance between proteinases and their inhibitors We investigated the expression patterns of matrix metalloproteinases (MMPs), tissue inhibitors of matrix metalloproteinases ... subcutaneous injections of 100 µg of mBSA (Sigma, Deisenhofen, Germany) in 50 µl of saline solution, emulsified in 50 µl of complete Freund's adjuvant (Sigma), adjusted to a concentration of mg/ml heat-killed...
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Báo cáo y học: "What do we know about communicating risk? A brief review and suggestion for contextualising serious, but rare, risk, and the example of cox-2 selective and non-selective NSAIDs" pot
... McGettigan P, Henry D: Cardiovascular risk and inhibitionof cyclooxygenase: a systematic review of the observational studies of selective and nonselective inhibitors of cyclooxygenase JAMA 2006, 296:1633-1644 ... set of data available for a single topic because the amount or extent of evidence is not available A notable exception is the case of NSAIDs and coxibs, and the outcomes of gastrointestinal and ... the subject of extensive investiga- Risk of serious skin reactions with coxibs [64] [64] tion in both randomised trials and a retrospective metaanalysis of them, and meta-analyses of substantial...
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Genetic polymorphisms of matrix metalloproteinases and their inhibitors in potentially malignant and malignant lesions of the head and neck potx
... gene expression of ECM and possible therapeutic aspects of MMPs and TIMPs in potentially malignant and malignant lesions of the head and neck Classification of MMP gene family and their substrates ... capable of degrading most components of the extra cellular matrix (ECM) [7-9] Degeneration of matrix is a key event in invasion and metastasis of malignant lesions of the head and neck Tissue inhibitors ... the protein levels Regulation of MMPs in potentially malignant and malignant head and neck lesions Polymorphism of MMPs in potentially malignant and malignant head and neck lesions The MMPs are...
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báo cáo khoa học: " Preclinical evaluation of KIT/PDGFRA and mTOR inhibitors in gastrointestinal stromal tumors using small animal FDG PET" ppsx
... survival of 12 weeks and a median overall survival of 34 weeks in a small series of patients pre-treated with imatinib and sunitinib [9] An in vitro and in vivo study on V561D-PDGFRA and D842VPDGFRA ... combinations, TKIs and m-TOR inhibitors [23] We studied the activity of everolimus as a new single agent and two combinations of agents, imatinib associated with nilotinib and imatinib associated ... to overcome the reduced affinity of the binding between imatinib and TK due to the acquisition of new mutations and to avoid the problem of an up-regulation of efflux transporters Nilotinib achieved...
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báo cáo khoa học: " Discovery of microvascular miRNAs using public gene expression data: miR-145 is expressed in pericytes and is a regulator of Fli1" pps
... kidney) and EBs with active sprouting angiogenesis (n = for both kidney and EB; error bars indicate standard error of the mean) stretch of basic amino acids in the carboxyl terminus of PDGF-B ... glomerulus and lung and this formed the basis of our selection (Additional data file 2) Among those with favorable scores in this analysis, miR-1263p and miR-126-5p (the two mature forms of miR-126) ... between fragments and surrounding tissue ± standard error of the mean (n = 4, 3, and for brain, muscle, skin and kidney, respectively) GAPDH, CD31 and VEGFR-2 (Flk1) TaqMan assays were used as...
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