Báo cáo Y học: Inhibition of SERCA Ca2+ pumps by 2-aminoethoxydiphenyl borate (2-APB) 2-APB reduces both Ca2+ binding and phosphoryl transfer from ATP, by interfering with the pathway leading to the Ca2+-binding sites ppt
Báo cáo Y học: Inhibition of SERCA Ca2+ pumps by 2-aminoethoxydiphenyl borate (2-APB) 2-APB reduces both Ca2+ binding and phosphoryl transfer from ATP, by interfering with the pathway leading to the Ca2+-binding sites ppt
... inhibition of SERCA (Eur. J. Biochem. 269) 3687 Inhibition of SERCA Ca2+ pumps by 2-aminoethoxydiphenyl borate (2-APB) 2-APB reduces both Ca2+ binding and phosphoryl transfer from ATP, by interfering with ... data to show that 2-APB can inhibit the SERCA Ca2+ pumps by reducing both the affinity of Ca2+ binding and phosphoryl transfer and postulate that the drugbinds to and interferes with the Ca2+entry ... M3, M4, M5 and M7. The binding of 2-APB to these sites could influence the movement of the loop between M6 and M7 (L6-7), and reduce access of Ca2+ to their binding sites. Keywords :2-APB; Ca2+-ATPase;...
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Báo cáo Y học: Inhibition of the SERCA Ca21 pumps by curcumin Curcumin putatively stabilizes the interaction between the nucleotide-binding and phosphorylation domains in the absence of ATP pot
... that the nucleotide -binding domain is highly mobile in the presence of Ca2þ and cancome into close contact with the phosphorylation site by simple thermal fluctuation [15]. From this type of analysis ... the absence and presence of curcumin, and controls to estimatenonspecific binding of ATP to the filter were performed asdescribed previously [16].Phosphorylation studiesPhosphorylation of the ... equation:½Eþ½L$½ELWhere [E] and [L] are the concentrations of free sites and ligands, respectively, and [EL] is the concentration of boundligand. The total concentration of sites can be expressed asN[E]0, the product...
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Tài liệu Báo cáo Y học: Inhibition of the MEK/ERK signaling pathway by the novel antimetastatic agent NAMI-A down regulates c-myc gene expression and endothelial cell proliferation ppt
... hypo-thesis is further confirmed by the observation that, differ-ently from the effect of serum, the stimulatory effect of PMA on ERK1/2 activity could also be totally abolished by NAMI-A. Within ... to the phosphorylation of ERK1/2 isoenzymes (Fig. 2B). To verify the involvement of a PKC-dependent pathway in both serum- and PMA-generated ERK1/2 phosphoryla-tion, the selective PKC inhibitor ... integrity and equal loading. The levels of radioactivity incorporated into c-myc product werenormalized by comparison with the levels of radioactivityincorporated into the GAPDH product from the...
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Tài liệu Báo cáo Y học: Inhibition of nuclear pre-mRNA splicing by antibiotics in vitro pot
... 2). The sixfold stron gersplicing inhibition by Cl-tetracycline may be explained by the a dditional s ize and hydrophobicity introduced by the substitution, as is often the case in ribozyme inhibition ... aminoglycoside,kanamycin, the a minocyclitol glycoside, streptomycin, t hepenicillins, ampicillin and penicillin G, the aminocyclitol,spectinomycin, tetracycline and Cl-tetracycline, and the macrolide, erythromycin) ... with the binding o f the functional sub strate.Type-II binding sites are the central metal ion -binding pock-ets i n the catalytic cores of ribozymes. In type-II binding sites the aminoglycosides...
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Báo cáo Y học: Inhibition of hyaluronan synthesis in Streptococcus equi FM100 by 4-methylumbelliferone doc
... contribute to their pathogenicity by allowingthem to escape from the immune systems of their hosts. The HA synthesized by Streptococci is not chemicallyor structurally distinguishable from that synthesized ... mechanism of inhibition of HA synthesis by MU isprobably due to an alteration of the lipid environment of the Streptococcal membranes.MATERIALS AND METHODSMaterialsLysozyme and MU were purchased from ... [31], and the results were confirmed by SDS/PAGE analysis of all the samples, according to the method of Laemmli [32].Assay of cell-free HA synthesisCell-free HA synthesis was performed by a modification...
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Báo cáo Y học: Inhibition of glycosyl-phosphatidylinositol biosynthesis in Plasmodium falciparum by C-2 substituted mannose analogues pot
... understanding of the biosynthesis pathway and function of GPtdIns came from the use of specific inhibitors of the GPtdInsbiosynthesis. A recently established fungi metabolite(YW3548) was shown to ... 2-deoxy-2-fluoro-D-glucose and 2-amino-2-deoxy-D-mannose) have beenused to study glycosylphosphatidylinositol (GPtdIns)biosynthesis and GPtdIns protein anchoring in protozoal and mammalian systems. The effects of these ... glucosamine into GPtdIns may point to an inhibition of GPtdIns biosynthesis by a mechanismwhich is different from the ones observed in othersystems, that is, the incorporation of mannosamine intothe...
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Báo cáo y học: "Extension of the PNA world by functionalized PNA monomers eligible candidates for inverse Diels Alder Click Chemistyr"
... night and the reaction’s completeness was checked by thin layer chromatography. The reaction prod-uct was inspissated by the rotary evaporator and consecu-tively und covered with ether. The ... Synthesis of the PNA building block backbone In the next step, the synthesis of the PNA back-bone monomer using the fluorenylmethoxycarbonyl (Fmoc) protection occurred as described by Atherton ... Atherton and Sheppard.[40] Synthesis of the Fmoc-C2-glycine-tert-butyl ester The synthesis of the peptide nucleic acid back-bone requires the introduction of protecting groups as shown in the...
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Báo cáo Y học: Characterization of the exopolysaccharide produced by Streptococcus thermophilus 8S containing an open chain nononic acid doc
... studies.ACKNOWLEDGEMENTSThis study was supported by the PBTS Research Program with financial aid from the Ministry of Economic Affairs and by the IntegralStructure Plan for the Northern Netherlands from the Dutch Develop-ment ... composition of the EPS produced by S. thermophilus 8S, the genetics and biochemistry of the EPS biosynthesis as well as the physical properties of the EPS will be intriguing subjects of further studies.ACKNOWLEDGEMENTSThis ... coevaporation with methanol, the mixture of partially methylated alditols was acetylated with acetic anhydride (3 h, 120 °C), and analyzed by GLC and GLC–EIMS [14,19].NMR spectroscopyPrior to NMR analysis,...
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Báo cáo khoa học: Inhibition of Drosophila melanogaster acetylcholinesterase by high concentrations of substrate potx
... used instead of the substrate to avoid decarbamoylation due to transcarb-amoylation by the choline, generated from the substratehydrolyzed by the noncarbamoylated fraction of the enzyme. Figure ... simultaneously to the free and the acetylated enzyme as shown by structuralstudies [30] and (b) the occupation of the anionic subsite at the bottom of the active-site blocks deacetylation as shown by our ... due to the replacement of the oxygen atom by a methylene group. The results were evaluated by fitting simultaneously the equation for decarbamoylation and the derived steady-stateequation to the...
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Báo cáo khoa học: Inhibition of a-synuclein fibrillization by dopamine analogs via reaction with the amino groups of a-synuclein Implication for dopaminergic neurodegeneration pot
... also retains the cytotoxicity, supporting the hypothesis that the cyto-toxicity primarily arises from the reaction adduct or the a-Syn oligomers rather than from free DA or the a-Syn fibrils. Although ... reactions of a-Syn with quinone and DA. (A) Overlay of the 1H-15N HSQC spectra of a-Syn (black) and the reaction product of a-Syn and Q (red). (B) Overlay of the 1H-15N HSQC spectra of a-Syn (black) ... (unpublished data). Study of inhibition of fibrillization may provide insight into understanding of the a-Syn fibrillization (Lewy-body formation) and the related cytotoxicity (dopaminergic loss)....
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