inhibitors of src family kinases
Tài liệu Báo cáo khoa học: Phosphorylation of cyclin dependent kinase 4 on tyrosine 17 is mediated by Src family kinases pptx
... unrelated Src family kinase inhibitors block the phosphorylation of CDK4 on Y17 As these inhibitors have similar activity against all Src family kinases [20,23], and we have shown that C-YES, C -SRC ... knockdown of C-YES or compensation by other Src family members It is known that Src family kinases share many substrates and show considerable functional redundancy [27], and it is likely the Src kinases ... Hospital Journal compilation ª 2008 FEBS 3103 Phosphorylation of CDK4 by Src family kinases A N G Martin et al A B B Fig Src family kinases phosphorylate CDK4 on Y17 in vitro (A) HeLa lysates (2.5...
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Tài liệu Báo cáo khoa học: TEC family kinases in health and disease – loss-of-function of BTK and ITK and the gain-of-function fusions ITK–SYK and BTK–SYK pptx
... agammaglobulinaemia is a member of the src family of protein-tyrosine kinases Nature 361, 226–233 Thomas JD, Sideras P, Smith CIE, Vorechovsky I, Chapman V & Paul WE (1993) Colocalization of X-linked agammaglobulinemia ... recipient of a PhD Fellowship from the Ministry of Higher Education and Scientific Research ⁄ KRG-Erbil, Iraq References Ortutay C, Nore BF, Vihinen M & Smith CI (2008) Phylogeny of Tec family kinases: ... a family of cytoplasmic enzymes that are important for several aspects of leukocyte biology Both loss- and gain -of- function mutations in humans have been instrumental in our understanding of...
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Báo cáo khoa học: Structural recognition of an optimized substrate for the ephrin family of receptor tyrosine kinases pot
... the selectivity of this peptide for EphA3 over other ephrin receptor kinases gives insight into substrate specificity for this biologically relevant class of receptor tyrosine kinases and provides ... general view of the EphA3:EPHOPT interface (C) The EphA3:OPTYF interface (PDB 3FY2) Compare the orientation of OPTYF residues Trp–4, Asn–3, Asp–2 and Glu+1 with those of EPHOPT in (B) C B of approximately ... addition, the backbone atoms of the Trp– Table Kinetic data The upper panel shows the effect of varying amino acids at the +2 position of the substrate The sequences of the tested peptides are...
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Báo cáo khoa học: Tec family kinases Itk and Rlk⁄ Txk in T lymphocytes: cross-regulation of cytokine production and T-cell fates pot
... TCR signaling Recognition of antigen major histocompatibility complex (MHC) by the TCR leads to a cascade of signaling events initiated by the activation of the Src- family kinase Lck, which phosphorylates ... amplification of expression of their master regulator GATA-3 For Th17 cells, transforming growth factor-b1 in the presence of IL-6 initiates differentiation of murine CD4 cells, leading to expression of ... regulators of cytokine production downstream of TCR stimulation Such studies reveal that mutation of the TFKs can profoundly influence the development, differentiation and function of cytokine-producing...
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Báo cáo khoa học: Tec family kinases: regulation of FceRI-mediated mast-cell activation ppt
... activation of the Src family kinase Lyn, which activates Syk, a member of the Syk ⁄ ZAP-70 kinase family This results in the phosphorylation of several tyrosine residues in LAT and the formation of a ... activation of the sarcoma (Src) family kinase Lyn, and subsequently to the activation of spleen tyrosine kinase (Syk), a member of the Syk ⁄ zeta-chain-associated kinase 70 (ZAP-70) kinase family ... version of Tec kinases to determine kinase-independent (i.e scaffolding) functions of Tec family members, because small molecule inhibitors for TFK have been developed [90– 92] Most of the studies...
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Báo cáo khoa học: Tec family kinases: Itk signaling and the development of NKT ab and cd T cells potx
... (2011) Tec family kinases: regulation of FceRI-mediated mast-cell activation FEBS J 278, 1990–2000 Schwartzberg P, Finkelstein L & Readinger J (2005) Tec -family kinases: regulators of T-helper-cell ... aspect of Itk, its role in the development and function of iNKT and NKT-like cd T cells Itk and i NKT cell development NKT cells are a subset of innate T cells characterized by their expression of ... Efficient selection of iNKT cells also depends on TCR signaling in response to cognate antigen in the context of CD1d Indeed, a number of signaling molecules that lie downstream of the TCR can affect...
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Báo cáo y học: "Differential expression of the FAK family kinases in rheumatoid arthritis and osteoarthritis synovial tissues" doc
... number of cells of a given type that reacted with a specific antibody divided by the total number of cells of that given type was defined as the percentage of reactivity The mean percentage of reactivity ... signaling molecules including Src and paxillin Formation of a Pyk2 -Src complex and the kinase activity of Src is required for bone resorption by osteoclasts [32] Src is highly phosphorylated in ... interaction and activation of Src family kinases [6] Our results demonstrate that unlike Src, paxillin and PLCγ, which are highly phosphorylated in RA ST lining, only low numbers of RA ST lining cells...
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Báo cáo y học: "Thioglycosides as inhibitors of hSGLT1 and hSGLT2: Potential therapeutic agents for the control of hyperglycemia in diabetes"
... notion of using SGLT inhibitors as a means to control circulating levels of glucose The selective inhibition of hSGLT2 by thioglycoside I, which is responsible for most of the reabsorption of glucose ... used to determine the amount of ATP in mg of protein measured from the number of cells per well After 24 h, the microtiter plate was taken for scintillation counting of radioactive [14C]AMG using ... comparison of SGLT1 and SGLT3 The Journal of Membrane Biology 2000; 176: 111-117 44 Santer R, Kinner M, Lassen CL, et al Molecular analysis of the SGLT2 gene in patients with renal glucosuria Journal of...
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Tài liệu Color Atlas of Pharmacology (Part 12): Inhibitors of the RAA System ppt
... Inexcitability Stimulus Rate of depolarization Suppression of AP generation Prolongation of refractory period = duration of inexcitability A Effects of antiarrhythmics of the Na+-channel blocking ... neurotransmitters The plasmalemma also harbors the sites of action of cardiac glycosides (the Na/K-ATPases, p 130), of Ca2+ antagonists (Ca2+ channels, p 122), and of agents that block Na+ channels (local anesthetics; ... degree of shortening, i.e., the force of contraction Sources of Ca2+ are: a) extracellular Ca2+ entering the cell through voltage-gated Ca2+ channels; b) Ca2+ stored in membranous sacs of the...
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Tài liệu Báo cáo khoa học: Functional and structural analyses of N-acylsulfonamidelinked dinucleoside inhibitors of RNase A ppt
... regarding a new class of surrogates for the phosphoryl group Results and Discussion Sulfonimides as inhibitors of RNase A We began by determining the ability of three backbone analogs of RNA to inhibit ... [60] Determination of Ki values Compounds 17 were assessed as inhibitors of catalysis of 6-FAMdArUdAdA6-TAMRA cleavage by RNase A [52,53] Briey, assays were performed in 2.00 mL of either 0.05 m ... N-Acylsulfonamide-linked dinucleosides as inhibitors of RNase A Given the efcacy of the sulfonimidyl group as a phosphoryl group surrogate, we sought to determine the advantage of adding nonbridging oxygens...
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Tài liệu VILLA ELSA A Story of German Family Life pdf
... unsightly colors, the clatter of the German home, gave further evidence of the absence of sensitiveness, of any fine and balanced poise of nerves This repulsiveness of existence, of course, did not affect ... everything on his side "This sort of thing, of course, kills the true[84] idea and fun of sport Take away its knightliness of bearing, spirit of self-sacrifice, exhibition of pluck though defeat is certain, ... through the illuminations of many profound and oracular professors in lofty pulpits He submitted that his German was too feeble of wing to enable him to soar into the heights of such wisdom The zest...
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Tài liệu Báo cáo khoa học: The capsid protein of human immunodeficiency virus: designing inhibitors of capsid assembly ppt
... belong to one of the following types: (a) non-nucleotide reverse transcriptase inhibitors; (b) nucleotide reverse transcriptase inhibitors; and (c) protease inhibitors [1] Because of the poorly ... side-effects of protease inhibitors in human fat metabolism [2], and the frequent emergence and spread of drug-resistant variants of HIV-1 [3], it is necessary to identify new types of drugs that ... shifts of the whole dimerization helix of CTD [27] (otherwise, those chemical shifts are too broad to be observed because of the presence of interconverting conformers) [29] The binding site of CTD...
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![Báo cáo khoa học: Calix[4]arene methylenebisphosphonic acids as inhibitors of fibrin polymerization doc](https://media.store123doc.com/images/document/14/rc/tp/small_tpb1394040066.jpg)
Báo cáo khoa học: Calix[4]arene methylenebisphosphonic acids as inhibitors of fibrin polymerization doc
... inhibitor of the final step of blood coagulation, fibrin polymerization, and can be used as the basis for the design of new class of antithrombotic agents We found that the mechanism of C-192 inhibition ... time of protofibril formation; Vmax, maximum rate of fibrin polymerization, which was defined by graphic calculation of the angle of the tangent to the turbidity increase curve at the point of maximum ... calixarene C-192 of both the thrombin–fibrinogen reaction and the re-association of fibrin desAABB indicates that calixarene retards clotting not as a result of the inhibition of thrombin, but...
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Báo cáo khoa học: Characterization of inhibitors of phosphodiesterase 1C on a human cellular system potx
... to the question of the validity of interpretations based on results obtained with the use of Characterization of inhibitors of PDE1C these compounds, especially as other modes of action besides ... modulation of ion currents [18–20] and adenosine receptor inhibition [21], respectively Because of the lack of a cellular model that allows separate monitoring of PDE1 activity, no comparison of the ... T R Dunkern and A Hatzelmann Characterization of inhibitors of PDE1C expressed in A172 cells, became inhibited Thus, the inhibition of these PDE family members might account for this effect Figure...
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Báo cáo khoa học: Structural and thermodynamic insights into the binding mode of five novel inhibitors of lumazine synthase from Mycobacterium tuberculosis pptx
... oxygen atoms of Ala59 and Glu61 of one subunit and with the main chain nitrogen of Asn114Â of the other subunit The contacts of the ribityl chain to His89 and Lys138Â are mediated by a net of water ... kcalặmol)1 for MbtLS TS50 The analysis of the thermodynamic parameters of the different inhibitors clearly showed an increase of the afnity (decreasing of DG) of the compounds bearing the alkyl phosphate ... The structural superposition of the pentamer- ic complexes with different inhibitors showed a highly conserved arrangement of the pentamers, independent of the nature of the inhibitor Lumazine (Fig...
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Báo cáo khóa học: Mutational and computational analysis of the role of conserved residues in the active site of a family 18 chitinase docx
... and formation of the oxazolinium ion intermediate; (C) Hydrolysis of the oxazolinium ion intermediate Copyright National Academy of Sciences, USA questioned on the basis of studies of chitinase ... Mutation of subsets of these conserved residues in various family 18 chitinases has shown for the majority that they are important for catalysis [20,26–31] However, the mechanistic roles of several of ... and there is no example of mutational analysis of all of these residues in the same enzyme To obtain an insight into how the many conserved residues in the active sites of family 18 chitinases contribute...
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Báo cáo khoa học: Halogenated benzimidazoles and benzotriazoles as inhibitors of the NTPase/helicase activities of hepatitis C and related viruses ppt
... again described only in patents [25] During the course of random screening of a wide range of unrelated compounds in a search for lead inhibitors of HCV NTPase/helicase activities, it was noted that ... benzotriazoles of the helicase activities of the enzymes from HCV, WNV, JEV and Suv3(D1–159), with use of a DNA substrate Helicase activity was determined as a function of increasing concentrations of the ... (IC50 of 1.5–5.5 lM) of the helicase activities of HCV, WNV and Suv3(D1–159), but not JEV The tetrachlorobenzotriazole TCBT is only a weak inhibitor of the HCV enzyme, and a moderate inhibitor of...
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STATEMENT OF INTENT: FAMILY MIGRATION pot
... Certificate of VAT registration and latest VAT return confirming VAT registration number if turnover in excess of £73,000 • Proof of ownership or lease of business premises • Proof of registration ... for the purposes of PAYE and National Insurance Proof of PAYE Reference Number and Accounts Office 48 Reference Number Evidence of registration must be original or certified copy of documentation ... their family life or leave to remain in the UK on the basis of their family or private life The rules will also reflect the fact that family life established when the parties knew one or both of...
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Báo cáo khoa học: Structure of FocB – a member of a family of transcription factors regulating fimbrial adhesin expression in uropathogenic Escherichia coli pdf
... FEBS 3369 Structure of FocB U W Hultdin et al moter-proximal regulatory genes [16,17] (Fig 1) One of these regulatory genes encodes the FocB protein, a member of the PapB family of fimbrial transcriptional ... atom of Leu23 and the side chain Oc1 atom of Thr83, and one hydrophobic interaction between the side chain of Leu18 and the Cc2 atom of Thr83 FocB dimerization Fig Ribbon representation of the ... Structure of FocB Fig Protein–DNA and –RNA complex structures of the top five structural homologs of FocB identified by DALI [38] Ribbon representations are shown to the left and overlays of Ca-traces of...
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Báo cáo khoa học: Structure, regulation and evolution of Nox-family NADPH oxidases that produce reactive oxygen species pptx
... post-translational regulation of Nox -family enzymes on the basis of three-dimensional structures and evolutionary conservation Structure of Nox -family enzymes Fig (A) A model for the structure of gp91phox Cylinders ... enzymes remains controversial [39,40] Origin of Nox -family enzymes There is no evidence for the presence of Nox, Fre or FRO in prokaryotes: a superfamily of flavocytochromes that transport electrons ... the NoxC subfamily emerged at a later stage of fungal evolution Thus, the classification of the Nox family in eukaryotes into the two major groups, depending on the presence or absence of the EF-hand...
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