biological activity and mechanism of action

... generation of H2O2 in spores [9,15–18] In this work we have gained more information on the cellular targets and the mechanism of action of vis- cotoxins, by examining the interaction of VtA3 with ... [3,16] To further explore the interaction of the most cytotoxic viscotoxin isoform, VtA3, with biological membranes and obtain information on its mechanism of action, we have applied different ... monochromator, and Glan-Thompson polarizers using quartz cuvettes with continuous stirring of the suspension, bandwidths of nm for excitation and nm for emission, and excitation and emission wavelengths of...

Ngày tải lên: 19/02/2014, 07:20

... target of NITD770 and hence, there was a need to determine its mode of mechanism During the studies to determine the mode of mechanism of NITD770, host lipid rafts (as suggested by chemogenomic profiling ... 68 3.2.4 Anti-viral activity of compound NITD448 73 3.3 DISCUSSION 75 A STUDY OF THE MODE OF ACTION OF NITD770, A SMALL MOLECULE INHIBITOR OF DENGUE VIRUS 79 4.1 ... Anti-viral activity profile of NITD770 in several assays 81 Table 4-2: Sequencing results of the genome of the NITD770 resistant viruses 91 Table 5-1: Effect of sterol inhibitors on DENV and HCV...

Ngày tải lên: 10/09/2015, 15:51

... comparison of transcriptome profiles of MV411 and THP-1 75 Figure 4.3 Hierarchical clustering of transcriptomic profiles of microarray data 78 Figure 4.4 Linear regression analysis of fold-changes of ... understanding the mechanism of action of drugs (Li, et al., 2007; Frolov, et al., 2003) (Nunoda, et al., 2007) Transcriptomic techniques can survey the expression levels of thousands of genes and ... Hyper activity of mTOR is known to promote cancer Rapa binds to mTOR by means of the FKBP12-rapa complex and inhibits the kinase action of mTOR This abrogates the phosphorylation of S6K1 and 4E-BP1,...

Ngày tải lên: 11/09/2015, 09:18

... and by FTC-MP-terminated DNA and HIV-1 RT in the presence of EFV This study furthers our understanding of the mechanism of action for anti-HIV drug interactions and the efficacy observed for ... Where and represent the individual action of drug or drug 2, while 1,2 represents the combined action of the drug combination The CI values of < 1, = 1, and > indicate synergy, additive effect, and ... indicated by the high peak of synergy above the flat plane of additivity (Fig 2A and 2B) and overall synergy volumes of 181 μM2% and 267 μM2%, respectively (Table 1) The combination of FTC+EFV was moderately...

Ngày tải lên: 12/08/2014, 23:21

... mellitus High levels of free radicals and the decline of antioxidant defense mechanisms lead to damage of cellular organelles and enzymes, increased lipid peroxidation, and development of insulin resistance ... effects on diabetes, hypertension and wound healing Presumably, one of mechanisms of action is its antioxidant activity The action of EPRT is to produce electrical pressure rather than an electrical ... continued to improve and heal, and her remaining gangrenous toes eventually fell off Her blood pressure at admission was 166/53 with use of Lisinopril, which was dropped and eventually ceased...

Ngày tải lên: 26/10/2012, 09:39

... markers [alkaline phosphatase (ALP) and sucrase-isomaltase] and the rate of proliferation, and by electron-microscopic examination As shown in Fig 1A, the levels of ALP and sucrase-isomaltase in RPMI ... affect biological and laser light scattering measurements, we first explored whether the presence of phosphate was necessary for the biological effect of CPP To this end, a first dose–response set of ... individual CPPs, b-CN(1–25)4P and as1-CN(59–79)5P, (A) and (C), respectively, and of a mixture of CPPs (CPP DMV) (B) Each point on the graphs corresponds to the mean value of the [Ca2+]i peak rise...

Ngày tải lên: 16/03/2014, 05:20

... inhibitory activity of this group of peptides is attributable to their effect on the turnover number of IN, and suggest a different mode of action from that of the rst group The third group of peptides, ... the Vmax and Kcat values; and peptides that bind IN, but have no effect on its activity Structural analysis of their interaction sites within IN provided insights into their mechanism of action ... protein on the basis of the RevIN interaction [55,5863] and following the use of a Rev-derived peptide library [58] With the use of a yeast two-hybrid (Y2H) system and a random peptide library,...

Ngày tải lên: 22/03/2014, 16:21

... neutrophils, and is a biomarker for inflammation Furthermore, to clarify the LA mechanism of action, we studied the participation of pentoxifylline, a PDE5 and TNF-alpha inhibitor, and morphine, a mu and ... pre-treatment of mice with LA (12.5 and 25 mg/kg, i.p) significantly reduced the volume (μL) of the edema in the 2nd (31 and 41%), rd (30 and 50%) and 4th (23 and 27%) hours after administration of dextran, ... light/dark cycle and food and water supplied ad libitum The experiments were carried out according to the Guide for the Care and Use of Laboratory Animals of the U.S Department of Health and Human Services...

Ngày tải lên: 11/08/2014, 03:20

... should be attached AND be politically adopted AND be of present interest AND contain clear and measurable aims Are there any plans of action aiming to promote physical activity and/ or healthy eating? ... municipalities and six town districts attached plans of action Of the attached documents, only seven policy documents and three plans of action from the municipalities, and five policy documents and one ... documents and plans of action, only 16 were of a high enough quality to be approved Discussion The main finding of this study was that policy documents and plans of action aiming to promote physical activity...

Ngày tải lên: 11/08/2014, 05:21

... filtration profile of FRK Crystal of SeMet FRK 3.4 Sample diffraction pattern of SeMet FRK crystal 81 3.5 Crystal structure of HoFRK 85 3.6 Structure based sequence alignment of HoFRK 90 3.7 Stereo ... and the actual UDP ligand Superimposition of one docked-ADP ligand and the actual ADP ligand Superimposition of the catalytic regions of the open SPS-F6P complex (cyan) and the closed SPS-S6PUDP ... (magenta) Schematic diagram of the reaction between F6P and UDP-Glc in the binding cleft of SPS A schematic diagram of the reaction involving FRK and Fructose Top a) SDS-GEL image of purified FRK Bottom...

Ngày tải lên: 11/09/2015, 09:08

... isopeptidase activity of colon cancer cells with an IC50 of approximately 50 µM.77 It induced Nrf2 activity of murine fibroblast cells at 20 µM69 and inhibited proteasomal activity of APL cells ... 5.3.3 Effects of 41, 219 and 227 on ER stress markers in NB4 cells 146 5.3.4 Effects of 41, 219 and 227 on the ER stress sensors PERK and IRE2 .148 5.3.5 Effects of 41, 219 and 227 on ... IC50 determination of curcumin and 41 on trypsin-, caspaseand chymotrypsin-like active sites of 20S proteasome 181 Appendix 4-2 Determination of substrates Km Initial rate of reaction containing...

Ngày tải lên: 11/09/2015, 14:20

... APQQEA HPLC chromatograms for reaction mixtures containing: (a) EDGFFKI and APQNEA, (b) MDC and APQNEA, (c) EDGFFKI and APNQEA, and (d) MDC and APNQEA, in the presence of tissue TGase after 60 incubation ... RGD and GFOGER (Knight et al., 1998; Knight et al., 2000), may result in the loss of full biological activity because of the absence of supplementary functional domains, such as synergy sites and ... diversity of collagen families makes development of a comprehensive, single model system challenging A system capable of emulating specific variables, such as the structure and biological activity, of...

Ngày tải lên: 12/09/2015, 08:20

... the point of receptor-ligand binding, upstream of Ras, upstream of Raf, and at the level of or downstream of Raf (Guy et al., 2003; Kim and Bar-sagi, 2004) The study conducted by Casci and colleagues ... representation of the Ras-ERK pathway induced by RTKs 1.3.1.3 The primary structure of Ras isoforms 12 1.3.1.4 Schematic representation of the primary structure of Raf 15 1.6.2 The structure and isoforms of ... Inhibition of the Ras-ERK signaling pathway by Spry 29 1.6.6 Points of action of Spry 30 1.6.6.1 Upstream of Ras 30 1.6.6.2 Upstream of Raf 32 1.6.7 Regulation of receptor ubiquitination and endocytosis...

Ngày tải lên: 14/09/2015, 14:06

... fragility and oxidative damage of erythrocytes of zinc-deficient rats J Nutr 1997; 127: 1290–1296 Lajos N, Miki N, Sandor S Protein and non-protein sulfhydryls and disulfides in gastric mucosa and ... spectrophotometric method [20] A mixture of 200 μL of 8% sodium dodecyl sulfate, 200 μL of 0.9% thiobarbituric acid and 1.5 ml 20% acetic acid was prepared 200 μL of RBCs lysate and 1.9 ml distilled water ... stress mechanisms Involvement of reactive oxygen species (ROS) has been demonstrated in the toxicity of many drugs to erythrocytes [7] PQ is used for treatment of malarial infections and its...

Ngày tải lên: 25/10/2012, 11:40

... by the action of cycloheximide Cycloheximide binds to the 80S-subunit of eukaryotic ribosomes and prevents the initiation and elongation reaction of protein biosynthesis The mycelium of pregrown ... cell-free extract and water to a final volume of 980 lL The reaction was started by the addition of 20 lL of a 100 mM ATP solution (final concentration mM) and the reduction of NAD was monitored ... heart, enzyme sample and water to a final volume of mL The reaction was started by addition of enzyme sample and decrease in absorbance at 340 nm was monitored One unit of enzyme activity was defined...

Ngày tải lên: 19/02/2014, 16:20

... clear activity zone of the cytoplasmic fraction (not shown) No activity on PGA was observed when the corresponding medium fraction was concentrated and similarly analysed Mode of action of PelB ... Hiromi K (1970) Interpretation of dependency of rate parameters on the degree of polymerization of substrate in enzyme-catalyzed reactions Evaluation of subsite afnities of exo-enzyme Biochem Biophys ... mapping On the basis of the assumptions of Hiromi [30] that the intrinsic rate of hydrolysis (kint) in the productive complex is independent of the length of the substrate, Km and Vmax were used...

Ngày tải lên: 20/02/2014, 03:20

... Scheme shows the reactions of the two-step mechanism of action of TFPI It is shown in the Appendix that Scheme is equivalent to Scheme I of [8] within the area of the applicability of the latter In ... values d and found the values of the hypothetical reactions separately The model of the inhibitory action of the Xa–TFPI complex on the enzyme–substrate complex (model 3) The reaction of X–VIIa–TF ... interaction verification Suppose that nM of VIIa–TF, nM of preformed Xa–TFPI, or 100 nM of Xa are mixed together and the factor VIIa–TF activity is monitored In the absence of Xa, slow inhibition of...

Ngày tải lên: 22/02/2014, 04:20

... a-helices Residues involved in binding of the cofactor ThDP are located at the C-terminal ends of the b-strands of Dom-c (diphosphates and Mg2+) and of Dom-a¢ of a neighbouring subunit (pyrimidine moiety) ... Dom-a and Dom-c of subunit A with their counterparts in subunit B It is stabilized by a large number of hydrogen bonds The weaker contact results from an association of Dom-a and Dom-b of subunit ... Superposition of the ThDP cofactors of BAL (grey), ALS (cyan), AHAS (green), IPDC (purple), BFD (yellow), CEAS (blue), POX (pink) and PDC (red) together with some residues important for cofactor binding and...

Ngày tải lên: 07/03/2014, 12:20