inhibition of the drug target enzymes—the desirable inhibition
Tài liệu Báo cáo khoa học: Substrate specificity and inhibition of brassinin hydrolases, detoxifying enzymes from the plant pathogens Leptosphaeria maculans and Alternaria brassicicola ppt
... both BHs The type of inhibition caused by cyclobrassinin was determined from the kinetics of inhibition of BHs, shown in the form of Lineweaver–Burk double reciprocal plots (Fig 8B,C) These results ... BHAb The temperature dependence of the activities of the BHs was tested in the range 5–56 °C; the apparent optimum temperatures of BHLmL2 were 25–30 °C FEBS Journal 276 (2009) 7412–7428 ª 2009 The ... and 85% inhibition of BHLmL2 and BHAb, respectively, while mm 2-mer- captoethanol caused 85% and 97% inhibition of BHLmL2 and BHAb, respectively The influence of pH on the activities of the BH...
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Tài liệu Báo cáo khoa học: Treatment of neutral glycosphingolipid lysosomal storage diseases via inhibition of the ABC drug transporter, MDR1 Cyclosporin A can lower serum and liver globotriaosyl ceramide levels in the Fabry mouse model doc
... disease, the primary pathology is in the kidney [1], the major site of Gb3 synthesis in man [11], and in the heart, possibly due to the association of Gb3 synthesis with the microvasculature GSL synthesis ... synthesis in the Fabry mouse model Our studies have further delineated the abnormal Gb3 synthesis in this model and have shown that the inhibition of MDR1 is a viable potential approach to the ... considered that the increased renal Gb3 of the Fabry mouse might extend to the glomerulus to provide a model of the human disease In the cortex of wild-type kidney, subpopulations of renal tubules...
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Báo cáo khoa học: Inhibition of the D-alanine:D-alanyl carrier protein ligase from Bacillus subtilis increases the bacterium’s susceptibility to antibiotics that target the cell wall potx
... and inhibition of the Dlt system was already present after the heterologous expression of the protein in E coli Kinetic analysis of the carrier protein modification by DltA Kinetic studies of the ... and Km The concentration of the inhibitor was plotted against the ⁄ cpm from the ATP ⁄ PPi exchange assays in Dixon plots [38] (Fig 4) The intersect of the three straight lines yields a Ki of 232 ... shows the specificity expected of this inhibitor Also, comparison of the Ki with the Km of DltA with d-Ala (13.62 lm; Fig 3), shows that the Ki is 60-fold lower which corroborates the suitability of...
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The NR4A orphan nuclear receptors are target genes of the novel drug c1 in cancer cells and potential mediators of drug induced apoptosis
... characterizes the role of nuclear receptors NR4A1 and NR4A3 in drug C1 mediated apoptosis and has identified the functional relevance of the increase in the transcript level of NR4A1 and NR4A3 This thesis ... that the decrease in VDAC1 protein levels in the mitochondria upon NR4A3 silencing corresponds to abrogation of apoptosis, but only when the drug dosage is low At higher doses of the drug the ... Accordingly, the great and urgent need presently is to investigate the role of each of the plenitude of genes and proteins important in the progression of cancer NUCLEAR RECEPTORS The nuclear...
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Tài liệu Báo cáo khoa học: The Arabidopsis protein kinase Pto-interacting 1-4 is a common target of the oxidative signal-inducible 1 and mitogen-activated protein kinases docx
... [17] On the other hand, expression of the tomato SlPti1 cDNA in the rice Ospti1a mutant suppressed the mutant phenotype These results indicate that PTI1 acts as a negative regulator of the HR ... Because the purified GST-MPKs showed autophosphorylation activity, loss -of- function (kinase-inactive) forms of the MAPKs were produced as GST-lofMPK3 and GSTlofMPK6 However, when lofMPK3 and lofMPK6 ... pathogen attack The Arabidopsis genome encodes 39 AGC kinases, of which 23 are classified to the AGC VIII group [8,9] The AGC kinases were named on the basis of their homology to the mammalian cAMP-dependent...
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Tài liệu Báo cáo khoa học: Mechanism of dihydroneopterin aldolase NMR, equilibrium and transient kinetic studies of the Staphylococcus aureus and Escherichia coli enzymes docx
... set of control data was obtained in the absence of the protein The data set obtained in the absence of the protein was then subtracted from the corresponding data set obtained in the presence of ... performed in the absence of the ligand The control data set obtained in the absence of the ligand was subtracted from the corresponding data set obtained in the presence of the ligand The Kd values ... cleavage of the bond between 1¢ and 2¢ carbons of the substrate The epimerization product is generated by the re-formation of the C–C bond after the reorientation of GA, which exposes the opposite...
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Tài liệu Báo cáo khoa học: Evolutionary relationships of the prolyl oligopeptidase family enzymes docx
... With respect to the studied enzymes of the POP family, POP seems to be the most conserved enzyme Ten conserved amino acids were found at the active site of the enzyme of each of the studied POP ... ACPH and DPP IV The whole bar and the lower part of the bar represent the similarity percentages of the catalytic domains and the complete sequences, respectively present in the last universal ... our analysis of subsite evolution, the specificity might be achieved by varying the structures of P2 and P3, but not the P1 subsite of the inhibitor The most interesting amino acid at the S3 subsite...
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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
... bromide stained gels of the reaction products obtained using lL of the RT products after 30 cycles of PCR amplification The lower part of panel A, and panels B, C report the expression of c-myc mRNA ... cells, indicating the capability of both drugs to selectively inhibit the PMA-dependent signaling leading to the phosphorylation of ERK1/2 isoenzymes (Fig 2B) To verify the involvement of a PKC-dependent ... expression To establish whether the decrease in c-myc mRNA expression elicited by NAMI-A might have occurred at the transcriptional level, we assessed the rate of transcription of the c-myc gene by using...
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Tài liệu Báo cáo khoa học: Cell surface heparan sulfate proteoglycans Target and partners of the basic ®broblast growth factor in rat Sertoli cells pptx
... USA) DNA quanti®cation The DNA content of the cell layer at the end of incubation was quanti®ed by the method of West et al [31] After solubilization of the cell layer in M NaOH and subsequent ... implication of cAMP increase, the second messenger of FSH, in the bFGF regulation was evaluated by addition to the culture medium of either mM dbcAMP or 10 lgámL)1 cholera toxin Their addition ... testicular development, the physiology of Sertoli cells is modi®ed The cell proliferation decreases and ceases allowing the establishment of the hematotesticular barrier around the 20th day postpartum...
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Tài liệu Báo cáo khoa học: The molecular surface of proteolytic enzymes has an important role in stability of the enzymatic activity in extraordinary environments pptx
... wild-type ALP I On the other hand, the Tm of D266N/Y269A-ALP I increased by only °C The denaturation temperature indicates the stability of the structure of the protein The difference of the increments ... surrounding residues of the depression, and the side chain of the mutated residue might restrain the mobility of the N-terminal region on the surface by interaction with the main chain of Lys26 by van ... wildtype enzyme, the side chain of Asp266 interacted with the amino group of the main chain at Glu268 The oxygen of the main chain at Asp266 was bound to amino groups of main chain of Tyr269 and...
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Tài liệu Báo cáo Y học: Evolution of the enzymes of the citric acid cycle and the glyoxylate cycle of higher plants pdf
... [106], these cases are relatively easy to explain as above But if one considers the evolution of all of the enzymes of the pathway (Fig 4), it is clear that only about half of the enzymes of the ... obtain an overview of the patterns of similarity for the enzymes of these pathways in plants and the relationships of their differentially compartmentalized isoenzymes Condensing the information ... to the cytosol of the host [3,83] For the tricarboxylic acid cycle, a complete transfer of the pathway to the cytosol would not work, because some of its enzymes are intergral components of the...
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Báo cáo khoa học: Substrate preference and phosphatidylinositol monophosphate inhibition of the catalytic domain of the Per-Arnt-Sim domain kinase PASKIN ppt
... translocation of UDPglucose pyrophosphorylase to the plasma membrane, where it increases cell wall glucan synthesis at the expense of glycogen storage In the absence of PSKs, glycogen rather than ... MEFs (data not shown) On the basis of the known functions of the PASKIN-related FixL oxygen sensor in bacteria and the PASKIN orthologues in yeast, and considering the lack of any obvious phenotype ... example of the results obtained after detection by phosphorimaging (B) Peptide sequences of the 30 most phosphorylated targets and their similarities to PKA and PKC consensus motifs (C) Target...
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Báo cáo khoa học: Analysis of the NADH-dependent retinaldehyde reductase activity of amphioxus retinol dehydrogenase enzymes enhances our understanding of the evolution of the retinol dehydrogenase family pot
... respectively [29] The overall analysis, examining the topology of the phylogenetic tree and the position of each gene inside the cluster, was informative regarding the orthology relationships of the distinct ... vertebrate enzymes The most significant difference between the amphioxus and the other retinal reductases was, nevertheless, their preference for the NADH cofactor To our knowledge, these are the first SDR ... that the N-terminal segment would be sufficient to target and anchor the protein to the ER membranes Furthermore, we analyzed the contribution of the C-terminal end to ER localization We fused the...
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Báo cáo khoa học: The Saccharomyces cerevisiae orthologue of the human protein phosphatase 4 core regulatory subunit R2 confers resistance to the anticancer drug cisplatin pot
... subunit of Pph3p required for the binding of Psy2p, we examined the sensitivity of the YBL046w ⁄ Psy4p deletion strain to cisplatin The comparable increased sensitivities to cisplatin of the homozygous ... identical to those of the wild-type cells Examination of the phenotype of S cerevisiae carrying deletions for both the YBL046w gene and the TUB2 gene Since decreased expression of Ppp4c in D melanogaster ... outside this region, the proteins are difficult to align because identity between the two proteins is low Nevertheless, the alignment in Fig shows that the overall similarity of the protein encoded...
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Báo cáo khóa học: Surface nucleolin participates in both the binding and endocytosis of lactoferrin in target cells potx
... inhibited the binding of HB-19-fluo to CHO 618 cells to an extent similar to that of the native hLf The noninvolvement of sequence 28RKVR31 of hLf was further confirmed by the lack of inhibition of HB-19 ... suggest that the C-terminal tail of nucleolin should be implicated in the mechanism of binding of Lf to nucleolin In general, the crosslinking of a ligand leads to the clustering or capping of its ... calculated from an overlay of the sensorgrams of all Lf concentrations using a method based on the Langmuir’s : binding model (BIAEVALUATION 3.1 software) Analysis of the inhibition of HB-19 binding to...
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Báo cáo khoa học: MR solution structure of the precursor for carnobacteriocin B2, an antimicrobial peptide fromCarnobacterium piscicola Implications of the a-helical leader section for export and inhibition of type IIa bacteriocin activity pdf
... help determine the structural basis of the inhibition of the antimicrobial activity of CbnB2 by the leader and to assist future analysis of the interaction of preCbnB2 with its ABC transporter ... for cleavage of the leader peptide after the double glycine motif [16,17] This cleavage occurs on the cytoplasmic side of the membrane during export of the bioactive peptide [18] The leader peptide ... establish the preferred geometry of the precursor We now report the chemical synthesis, biochemical production, and solution structure of preCbnB2, and compare it with the structure of the mature...
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Báo cáo khoa học: Kinetics of the inhibition of neutrophil proteinases by recombinant elafin and pre-elafin (trappin-2) expressed in Pichia pastoris ppt
... further characterized To limit the appearance of the 13 kDa clipped form of trappin-2 for the large-scale production of trappin-2, the duration of fermentation was reduced to three days Under these ... 0.02 s)1 for the inhibition of PR3 by 1.6 lM rectrappin-2 Accurate values of kdiss could not be calculated using Eqn (4) because of the almost complete inhibition of HNE and PR3 once the steady ... regression analysis of the data using Eqn (7) and using the best estimate of kdiss governing the dissociation of the HNErecelan complex Good ts were also obtained for the three other enzymeinhibitor...
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Báo cáo Y học: Modulation of the oligomeric structures of HIV-1 retroviral enzymes by synthetic peptides and small molecules pptx
... vitro In these authors’ opinions, such studies obviously represent the next logical step in the unfolding story of the modulation of the oligomeric structures of HIV-1 viral enzymes by synthetic ... aminoacid residues at the N- and C-termini of PR contribute close to 75% of the total Gibbs energy [15] The importance of this four-stranded b sheet is further emphasized by the fact that all PR ... N-terminus of the peptide [20] The development of these Ômore potentÕ peptide inhibitors firmly established that PR dimerization was a rational target for the development of AIDS therapeutics,...
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Báo cáo Y học: Baboon cytochrome P450 17a-hydroxylase/17,20-lyase (CYP17) Characterization of the adrenal microsomal and cloned enzymes docx
... [3,4] The dual activity of CYP17 and the differential regulation thereof have been the subject of many studies It is apparent that the normal expression and dual hydroxylase and lyase activities of ... Before the addition and (B) after the addition of NADH to the reference cuvette The reduction in the peak at 425 nm after addition of NADH is indicative of the presence of cytochrome b5 (C) NADH reduced ... respect to the interaction of the enzyme with the 17-hydroxylated intermediate Baboon CYP17 initially converted most of the PREG to 17-OHPREG and during the entire experiment, the ratio of DHEA/17-OHPREG...
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Báo cáo khoa học: Inhibition of the NF-jB transcriptional activity by protein kinase A pot
... abolish the inhibitory effect of PKA on NF-jB (Fig 5B) In this study, we have demonstrated the evidence that the C-terminal transactivation domain of p65 is responsible for the inhibition of NF-jB ... conflicting evidences regarding the action of PKA on the NF-jB activity Although the majority of reports [10–14] including this study, demonstrated the inhibitory actions of PKA on the NF-jB dependent gene ... inhibit TNFa-induced DNA-binding of NF-jB (Fig 3D) Thus, it is likely that the inhibitory effect of PKA on NF-jB is not due to the inhibition of DNA-binding activity of NF-jB PKA activation does...
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Tìm thêm: hệ việt nam nhật bản và sức hấp dẫn của tiếng nhật tại việt nam xác định các nguyên tắc biên soạn khảo sát chương trình đào tạo gắn với các giáo trình cụ thể tiến hành xây dựng chương trình đào tạo dành cho đối tượng không chuyên ngữ tại việt nam điều tra đối với đối tượng giảng viên và đối tượng quản lí điều tra với đối tượng sinh viên học tiếng nhật không chuyên ngữ1 khảo sát thực tế giảng dạy tiếng nhật không chuyên ngữ tại việt nam nội dung cụ thể cho từng kĩ năng ở từng cấp độ xác định mức độ đáp ứng về văn hoá và chuyên môn trong ct đặc tuyến hiệu suất h fi p2 đặc tuyến mômen quay m fi p2 đặc tuyến tốc độ rôto n fi p2 đặc tuyến dòng điện stato i1 fi p2 động cơ điện không đồng bộ một pha sự cần thiết phải đầu tư xây dựng nhà máy thông tin liên lạc và các dịch vụ phần 3 giới thiệu nguyên liệu từ bảng 3 1 ta thấy ngoài hai thành phần chủ yếu và chiếm tỷ lệ cao nhất là tinh bột và cacbonhydrat trong hạt gạo tẻ còn chứa đường cellulose hemicellulose chỉ tiêu chất lượng theo chất lượng phẩm chất sản phẩm khô từ gạo của bộ y tế năm 2008 chỉ tiêu chất lượng 9 tr 25