kinase inhibitor selectivity profiling using differential scanning fluorimetry

Ngày tải lên: 12/01/2014, 22:19

... and downregulation in TGM2 (Figure 1) Evaluation by qPCR using validation cell lines We evaluated the expression profiling of the 19 genes using four validation cell lines (RERF-LC-MS [AD], LC1/sq ... cancer cell lines using a statistical processing method, PCA, which is based on gene expression profiling determined by qPCR Four subtypes were optimally classified by PCA using 12 genes (AMY2A, ... components 1, 2, and (PC1, PC2, and PC3; dimensions) shown in Figure 2(A) Using the same frame, the four subtypes were also classified using all 12 test and validation cell lines, as shown in Figure 2(B)...

Ngày tải lên: 15/02/2014, 04:20

... differences in these values Differential scanning calorimetry DSC experiments were performed on a Calorimetry Sciences Corporation (CSC) 6100 Nano II differential scanning calorimeter with a ... spectrophotometrically using an excitation coefcient e280nm ẳ 30 ã 103 M)1ặcm)1 [15] The activity of the proteins was checked using the Tc titration method The concentration of Tc was determined in 0.1 M HCl using ... dierential scanning calorimetry Annu Rev Phys Chem 38, 463488 20 Takahashi, K & Sturtevant, J.M (1981) Thermal denaturation of Streptomyces subtilisin inhibitor, subtilisin BPNÂ, and the inhibitorsubtilisin...

Ngày tải lên: 20/02/2014, 02:21

... Sunderland, United Kingdom Section Application of Differential Scanning Calorimetry into Pharmaceuticals Chapter Application of Differential Scanning Calorimetry to the Characterization of Biopolymers ... differential scanning calorimetry (DSC) under the nitrogen flow, using the second heating cycle Molecular weight properties were determined by a gel permeation chromatography (GPC) with the using ... – Differential Scanning Calorimetry, Isothermal Titration Calorimetry and Microcalorimetry, Edited by Amal Ali Elkordy p cm ISBN 978-953-51-0947-1 Contents Preface IX Section Application of Differential...

Ngày tải lên: 06/03/2014, 22:20

... protein kinase inhibitor of cAMPdependent protein kinase J Biol Chem 272, 18169–18178 Gamm, D.M & Uhler, M.D (1995) Isoform-specific differences in the potencies of murine protein -kinase inhibitors ... an inhibitor protein of cAMP-dependent protein kinase J Biol Chem 266, 11158–11162 Scarpetta, M.A & Uhler, M.D (1993) Evidence for two additional isoforms of the endogenous protein kinase inhibitor ... cAMP-dependent protein kinase in mouse J Biol Chem 268, 10927–10931 Olsen, S.R & Uhler, M.D (1991) Inhibition of protein kinase- a by overexpression of the cloned human protein -kinase inhibitor Mol Endocrinol...

Ngày tải lên: 07/03/2014, 15:20

... F-actin were also examined in these experiments Differential scanning calorimetry (DSC) DSC experiments were performed on a DASM-4M differential scanning microcalorimeter (Institute for Biological ... differential scanning calorimetry Eur J Biochem 267, 1869–1877 Golitsina, N.L., Bobkov, A.A., Dedova, I.V., Pavlov, D.A., Nikolaeva, O.P., Orlov, V.N & Levitsky, D.I (1996) Differential scanning calorimetric ... aliquots were taken and analysed by SDS/ PAGE [31] Digestion was terminated by adding soybean trypsin inhibitor at a 1.5 : (w/w) ratio to trypsin The proteins were dialyzed against 30 mM Hepes, pH 7.3,...

Ngày tải lên: 17/03/2014, 10:20

... conditions using the interior product Section VIII provides a summary of the main points made in the paper WARNICK, SELFRIDGE, AND ARNOLD: DIFFERENTIAL FORMS February 12, 1997 II Differential ... reformulated using di erential forms The authors have developed a convenient representation of electromagnetic boundary conditions 18] Thirring 17] treats several applications of EM theory using forms ... Poynting's Theorem Using Maxwell's laws, we can derive a conservation law for electromagnetic energy The exterior derivative of S is dS = d(E ^ H ) = (dE ) ^ H ? E ^ (dH ) Using Ampere's and...

Ngày tải lên: 24/04/2014, 16:51

... increasing the scanning rate increases sensitivity, while decreasing the scanning rate increases resolution to obtain thermal event temperatures close to the true thermodynamic value, slow scanning ... controlled temperature programme1 – mass is lost if the substance contains a volatile fraction Differential Scanning Calorimetry (DSC) – provides information about thermal changes that not involve ... thermal analysis Theory of thermal analysis techniques – Thermal Gravimetric Analysis (TGA) – Differential Scanning Calorimetry (DSC) Generating valid data – Calibration – Sample preparation Interpreting...

Ngày tải lên: 24/05/2014, 20:41

... Dasatinib, a multi-target tyrosine kinase inhibitor, targets Src kinase, in addition to BCR-Abl, c-KIT, PDGFR and ephrin-A receptor kinases It is the most potent Src kinase inhibitor currently in clinical ... EphA2 kinase EphA2 IP: p-EphA2 FAK kinase p-FAK py861 p-FAK py397 α-tubulin 48 Hr 24 Hr Hr Hr 0.5 Hr C C EphA2 IP: EphA2 kinase EphA2 IP: p-EphA2 Figure IPblotting for Src kinase, phospho-Src kinase ... A Src kinase p-Src py418 EphA2 IP: EphA2 kinase EphA2 IP: p-EphA2 FAK kinase p-FAK py861 α-tubulin B HT144 - Lox-IMVI + - Malme-3M Sk-Mel-5 Sk-Mel-28 - + - + - + + Dasatinib 100 nM Src kinase...

Ngày tải lên: 18/06/2014, 15:20

... scanned from left to right and moved from bottom to top of the image After a thermal drift reducing, using the STM tip, we applied voltage ‘from a reverse bias to a forward bias’ The time of applying ... ?0.4 V White circles shown in Fig indicate hole structures (width: 15–18 nm, depth: 0.9–1.1 nm), using it as markers for confirming a same position By the repetition of applying voltage as shown ... at the particular sites (substrate temperature: 430°C) White circles indicate hole structures, using it as markers for confirming the same position a Before, b and c during applying voltages,...

Ngày tải lên: 21/06/2014, 08:20

... Thermal Transitions on Cooling of Rice Starch 38 INTRODUCTION Differential scanning calorimetry (DSC) is a technique commonly employed to probe thermal properties of ... measurements were performed in duplicate Heat flow and temperature were calibrated using pure indium Data analysis was carried out using the Thermal Advantage Q series Q100-0021 (TA Instruments Inc., New ... (1991) Exothermic transitions in whole grain milled rice and milled rice flour studied by differential scanning calorimetry Cereal Chem., 68, 606–609 Vasanthan, T & Hoover, R (1992) Effect of...

Ngày tải lên: 07/08/2014, 14:20

... the nuclear factor (NF)-κB signal transduction pathway [9] Phosphorylation of inhibitor of κB (IκBα) by the IκB kinase (IKK) complex is a crucial step in NF-κB/Rel activation The IKK complex ... independent experiments performed in triplicates (*p < 0.01) IKK-β-targeted NF-κB blockade using a small peptide inhibitor ameliorates synovial inflammation, both in an animal model of arthritis and ... were lysed and total intracellular protein was separated using SDS-PAGE After immunoblotting, ph- and unphosphorylated IκBα were detected using specific mAbs NBD pre-treatment resulted in reduced...

Ngày tải lên: 09/08/2014, 08:22

... genes was performed using the ABI Prism 7900HT sequence detection system (Applied Biosystems (Foster City, CA, USA) Metalloproteinase and inhibitor expression were determined using SYBR Green (Takara ... gelatinases, no inhibitory activity was detected in IL-1+OSM media after day 10 (Figures and 3) Gene expression analysis reveals the differential levels of metalloproteinase and inhibitor transcripts ... that showed that either a furin-like enzyme inhibitor, Dec-RVKR-CH2Cl, or the general trypsin-like serine proteinase inhibitor, alpha1-proteinase inhibitor, can block the activation of pro-collagenases...

Ngày tải lên: 09/08/2014, 08:22

... or c-Met expression using ribozyme radiosensitizers in GBM cells in vitro and xenograft tumor in vivo [10], demonstration of clinically useful inhibitors of the tyrosine kinase activity of c-Met ... by using confocal microscopy Median intensity of each cell was calculated using Photoshop and a sided t-test was used to calculate the difference Comet assay dsDNA breaks were visualized by using ... have not been previously tested in GBM models In the work presented here, a novel inhibitor of c-Met tyrosine kinase, MP470 [11], was tested for its ability to radiosensitize GBM cells both in...

Ngày tải lên: 09/08/2014, 10:20

... and 1.50° for rater with digital scanning and 5.27° and 3.08° respectively with neutral suspension casting The SRD with digital scanning of Discussion Digital scanning and neutral suspension casting ... Suspension Casting Digital Scanning Overall, we found excellent intra and inter-rater reliability with low SEM values for measurement of the six parameters using digital scanning within both raters ... calculated using SPSS Inter-rater reliability The results for the inter-rater reliability analysis ICC, 95% confidence intervals and SEM values, for neutral suspension casting and digital scanning...

Ngày tải lên: 10/08/2014, 21:24

... nonrelated tyrosine kinase (Table 1) [18] The selectivity profile of ABT-869 against a broader range of kinases is illustrated in Figure In comparison to other multitargeted RTK inhibitors (PTK787 ... http://www.jhoonline.org/content/2/1/33 Figure Kinase inhibition profile of ABT-869 against a broader range of kinases Kinase inhibition profile of ABT-869 against a broader range of kinases Nonclinical in vivo ... inhibited a broader number of kinases relevant to the VEGF signaling pathway AG013736, CHIR258, and SU11248 are also active against most of the targeted kinases but these inhibitors demonstrate more...

Ngày tải lên: 10/08/2014, 22:20

... phosphatidylinositol 3 -kinase inhibitor J Natl Cancer Inst 2006, 98:545-556 30 Kong D, Yamori T: ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol kinase isoforms Cancer ... Phosphatidylinositol 3 -kinase inhibitors: promising drug candidates for cancer therapy Cancer Sci 2008, 99:1734-1740 32 Kong D, Yaguchi S, Yamori T: Effect of ZSTK474, a novel phosphatidylinositol 3 -kinase inhibitor, ... especially PI3-Kδ [30] A PI3-Kδ-selective inhibitor, IC87114 (1 μM), completely inhibited OC formation, while a PI3Kγ-selective inhibitor, AS605240, had no inhibitory effect Table 1: Histological...

Ngày tải lên: 12/08/2014, 12:20

... LAR We demonstrate that there is a differential role of Rho -kinase in the agonistinduced airway obstructions and that inhalation of the specific Rho -kinase inhibitorY-27632 results in a strong ... dependent on Rho -kinase for its contractile effect Conclusion Inhalation of the Rho -kinase inhibitor Y-27632 causes a considerable bronchoprotection to histamine and PGF2α Moreover, a differential ... inhalation of the Rho -kinase inhibitor Y- 27632 reverses the AHR to both agonists after the allergen-induced EAR and LAR The results strongly indicate that an increased Rho -kinase activity is involved...

Ngày tải lên: 12/08/2014, 16:20

... found using a larger value of α contains more features with strong relevance to the target class concept, but also more redundancy among these features Conversely, a predictor set obtained using ... found using the Page of 21 (page number not for citation purposes) Algorithms for Molecular Biology 2007, 2:7 DDP-based feature selection technique and simple but illustrative examples using ... set which is obtained using the DDP ∗ value of α MP shows enhanced separation of classes in PC space compared to separation of classes in the original feature space (measured using the Manhattan...

Ngày tải lên: 12/08/2014, 17:20