structure based design of potent glycogen phosphorylase inhibitors
Tài liệu Báo cáo khoa học: Crystal structure of Trypanosoma cruzi glyceraldehyde-3-phosphate dehydrogenase complexed with an analogue of 1,3-bisphospho-D-glyceric acid Selective inhibition by structure-based design docx
... results of these studies were confirmed by site-directed mutagenesis of specific residues of the two sites Secondly, model building of the best inhibitors based on the refined structures of the two ... Inhibition of T cruzi gGAPDH Inhibitor design All structures of 1,3-BPGA analogues are given in Table Inhibitors were designed from the reference compound 2-oxo-1,5-diphosphonopentane (5); its structure ... rendered the mechanistic approach and the design of inhibitors such as 1,3-BPGA analogues far from easy Indeed, the most potent and selective inhibitors of gGAPDH from parasites (T brucei, Leishmania...
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STRUCTURE AND REGULATION OF YEAST GLYCOGEN SYNTHASE
... INTRODUCTION A Glycogen Structure of glycogen Glycogen, a branched polymer of glucose serves as one of the major repositories of carbon and energy in eukaryotes The linear polymerization of glycogen ... degradation of glycogen Synthesis of glycogen polymer involves the activity of the glycogenin, glycogen synthase and branching enzyme Degradation of the polymer is mediated by glycogen phosphorylase ... generation of ATP or the biosynthesis of glycogen Insulin dependent inhibition of glycogen synthase kinase (GSK3) and dephosphorylation of GS by protein phosphatases promote the synthesis of glycogen1 2-14...
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Tài liệu Báo cáo khoa học: "DESIGN OF A KNOWLEDGE-BASED REPORT GENERATOR" doc
... selection of appropriate anaphora for subject phrases 4) morphological processing of verbs; 5) interjection of appropriate punctuation; and 6) control of discourse mechanics, such as inclusion of more ... ) This production infers that if the closing status of the Dow had a direction of "up', and yet the number of declines exceeded the number of advances for the day, then it can be said that the ... constructs of the system are of two types: 1) static knowledge structures, or memory elements, which can be thought of as ndimensional propositions, and 2) dynamic knowledge structures, or production...
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Báo cáo khoa học: Design of expression vectors for RNA interference based on miRNAs and RNA splicing potx
... expense of failure of cleavage of primiRNA by Drosha [8,9] In contrast and in summary, the RNAi expression vectors we describe here, pSM155 and pSM30, which are designed based on knowledge of miRNA ... vectors generate efficient knockdown of target proteins To examine the efficiency of generation of RNAi for pSM155 and pSM30, we examined the knockdown of expression of firefly Luciferase (Luc) HeLa cells ... artificial miRNA [4,6,7] An example of this design is shown in Fig 1A [4] As shown, the pri-miRNAs based on miR155 are processed in the nucleus by Drosha to set up transport of pre-miRNAs to the cytoplasm,...
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Báo cáo khoa học: Structure–function relationship of novel X4 HIV-1 entry inhibitors – L- and D-arginine peptide-aminoglycoside conjugates pptx
... responsive element (TAR) RNA binding, NMR structures of TAR–ligand complexes and aminoglycoside–RNA interactions, we have designed and synthesized a set of conjugates of aminoglycoside antibiotics with ... (6- and 9-mers), would lead to more potent HIV1 inhibitors than a manifold of arginine conjugated via the amino groups of the aminoglycosides Thus, a new set of poly arginine 6-mer and 9-mer d- ... spectrometry The second step of the synthesis involved full protection of the remaining amino groups with Cbz, achieved by the reaction of benzylchloroformate (CbzCl) in the presence of sodium carbonate...
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Báo cáo khoa học: Template-assisted rational design of peptide inhibitors of furin using the lysine fragment of the mung bean trypsin inhibitor pptx
... trypsin, the Lys fragment of MBTI may also serve as an ideal template for the design of potent, specific and stable furin inhibitors Here we report the design and synthesis of various peptide analogs ... SFTI-1, as one of the smallest peptide -based natural trypsin inhibitors, has shown significant potential to be used as a template molecule for the design of specific inhibitors to target biomedically ... models based on the crystal structures of furin and kexin: explanation of their specificity J Mol Biol 345, 211–227 Song HK, Kim YS, Yang JK, Moon J, Lee JY & Suh SW (1999) Crystal structure of a...
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Báo cáo khoa học: The structural comparison of the bacterial PepX and human DPP-IV reveals sites for the design of inhibitors of PepX activity pot
... (2005) 2050–2059 ª 2005 FEBS Sites for the design of inhibitors of PepX activity A B C D Fig Structures of enzymes of the clan SC The N-terminal domain of each enzyme is colored red, the catalytic ... active site of: (A) the crystalline structure of PepX from L lactis; (B) the modeled structure of PepX from S gordonii (C) Structure of PepX from S gordonii (orange) computed by MODELLER software, ... active site of the modeled structure of PepX from S gordonii c B C D 2055 Sites for the design of inhibitors of PepX activity but this does not seem to be essential for the binding of valine-pyrrolidide...
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Báo cáo khoa học: "Corpus-Based Induction of Syntactic Structure: Models of Dependency and Constituency" pdf
... systems that we are aware of operate under the assumption that the probability of a dependency structure is the product of the scores of the dependencies (attachments) in that structure Dependencies ... ordered (head, dependent) pairs of words, but the score of a dependency can optionally condition on other characteristics of the structure, most often the direction of the dependency (whether the ... in September (a) Classical Dependency Structure fell IN in September (b) Dependency Structure as CF Tree (c) CFG Structure Figure 1: Three kinds of parse structures speech categories may be included...
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Báo cáo Y học: Synthesis, conformational analysis and biological activity of cyclic analogs of the octadecaneuropeptide ODN Design of a potent endozepine antagonist pot
... Characterization of the secondary structure of these two ligands of ODN receptors should provide useful information for the design of potent, stable and selective agonists and antagonists of these receptors ... vicinity of cultured cells provoked a wave of calcium in the cytoplasm of astrocytes (Fig 3A) while ejection of culture medium alone had no effect (Fig 3B) Comparison of the amplitude of the response ... FEBS 2001 Design of a potent endozepine antagonist (Eur J Biochem 268) 6049 Fig RP-HPLC monitoring of N- and C-terminal deprotections and on-resin cyclization of the linear precursor of cyclo128...
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Báo cáo khoa học: Increased sensitivity of glycogen synthesis to phosphorylase-a and impaired expression of the glycogen-targeting protein R6 in hepatocytes from insulin-resistant Zucker fa ⁄ fa rats pptx
... inactivation of glycogen synthase and inhibition of glycogen synthesis The rate of glycogen synthesis, but not the activity of glycogen synthase, inversely correlated with the activity of phosphorylase- a ... determination of glycogen synthesis and the activities of phosphorylase- a and glycogen synthase (A) Phosphorylase- a (B) Active glycogen synthase versus phosphorylase- a (C) Glycogen synthesis versus phosphorylase- a ... determination of glycogen synthesis and the activities of phosphorylase and glycogen synthase as in Fig (B) Active glycogen synthase versus phosphorylase- a (C) Glycogen synthesis versus phosphorylase- a...
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functional discourse grammar a typologically-based theory of language structure sep 2008
... expression of underlying structures is potentially based on information from all higher levels, not just from the next one up Having seen something of the architecture of FDG and of its implementation ... proposed the idea of a Functional Discourse Grammar At the time it was conceived of as a revised version of Functional Grammar (FG; Dik 1997a, 1997b), a theory of the organization of natural languages ... morphosyntactic level of analysis, all of them with hierarchical layering; the actional status of ascription and reference; the top-down operation of the model; the interaction of the grammatical...
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Báo cáo hóa học: " Design of zone-based bandwidth management scheme in IEEE 802.16 multi-hop relay networks" doc
... next time of BS bandwidth allocation Intra-zone handoff and inter-zone handoff Moreover, by introduction the idea of zone, two types of handoff between RSs are defined, intra-zone handoff and inter-zone ... re-allocation is not necessary for handoffs of the user among the RSs of the same zone as displayed in Figure The size of a zone is defined to be the hop count of the most distant RS from the initial ... decrease in network utilization For designing QoS mechanisms, most of the Centralized -based research works [20,21] focused on the construction of the routing tree based on different QoS types Distributed...
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Báo cáo hóa học: " Research Article System-Platforms-Based SystemC TLM Design of Image Processing Chains for Embedded Applications" potx
... hardware-software partitioning, system parameters tuning, and design of specific hardware accelerators This makes the reuse of platform -based designs easier than specific designs GENERAL VEHICLE DESIGN ... relatively old technique for software development that uses component -based software design to accelerate the software development process [13, 14] On another side, UML -based design flows [15–21] have ... between embedded software design, architecture, intermicrocontroller communication and implementation This flattening of the design process can be best managed through platform -based design at the...
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neural network based adaptive controller design of robotic manipulators with an observer 88 doc
... controller–observer design based on passivity defined in theory where the unstructured uncertainty (6) is not considered for the time being SUN et al.: NEURAL NETWORK -BASED ADAPTIVE CONTROLLER DESIGN 57 ... special case of the one presented in Theorem with SUN et al.: NEURAL NETWORK -BASED ADAPTIVE CONTROLLER DESIGN 59 Fig Adaptive controller with an observer C Observer -Based Controller Design Using ... requirements of tracking accuracy and controller stability, so that the best performances of these two types of controllers can be compared In order to check the impact of the approximation power of these...
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Báo cáo y học: "Quantification of the glycogen cascade system: the ultrasensitive responses of liver glycogen synthase and muscle phosphorylase are due to distinctive regulatory designs" pptx
... example of such an enzyme cascade system is the regulation of glycogen phosphorylase (GP) and glycogen synthase (GS), enzymes involved in glycogen degradation (glycogenolysis) and synthesis (glycogenesis) ... provided experimental proof of zero order ultrasensitivity in the muscle glycogen phosphorylase cascade Theoretical analysis of the glucose-induced switch between phosphorylase and glycogen synthase ... modification of enzymes at various concentration of glucose The sensitivity of the fracApp App tional dose-response curve of glycogen synthase (curve a, ηH ~13.6), phosphorylase (curve b, ηH ~6.3), phosphorylase...
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Analysis and design of ship structure
... optimum design may be different from the owner optimum design 18.2.1 Rationally Based Structural Design versus Rules -Based Design There are basically two schools to perform analysis and design of ... their structural design But, even with the development of numerical techniques, design still remains based on the designer’s experience and on previous designs There are many designs that satisfy ... examined 18.2.3 Preliminary Design versus Detailed Design For a ship structure, structural design consists of two distinct levels: the Preliminary Design and the Detailed Design about which Hughes...
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Computer aided drug design of neuraminidase inhibitors and MCL 1 specific drugs
... R292K mutation 87 5.2.4 Comparison of the poses of potential inhibitors with wild strains 88 5.2.5 Comparison of the poses of potential inhibitors with mutant strains 91 Chapter ... absence of the target structure, lead discovery can be divided into two major class i.e ligand -based lead discovery and structure- based lead discovery 1.3 Ligand and Structure based drug design ... availability of structural information of the target, CADD can be divided into two categories (Figure1.3) i.e ligand -based and structurebased CADD Structure- based CADD relies on the knowledge of the...
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Structure function relationships of variegin a novel class of thrombin inhibitors
... n-variegin and its Ki 77 2.3.2.3 Design of deletion variants 79 2.3.2.4 Synthesis of s-variegin and variants 80 2.3.2.5 Selectivity profile of variegin 80 2.3.2.6 Inhibition of thrombin amidolytic 84 ... groups of naturally occurring thrombin inhibitors, thus belongs to a new class of its own A wide selection of peptides with different potencies, kinetics, mechanisms of inhibition were designed ... Pictures of Amblyomma variegatum 55 Figure 2.3 Purification of variegin isoforms by RP-HPLC 72 Figure 2.4 Amino acid sequence of variegin and isoforms 76 Figure 2.5 Michaelis-Menten constant (Km) of...
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