iv— inhibitors of crystallization
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 ... to search for putative inhibitors of PepX, using the knowledge of DPP-IV inhibition as a starting place We thus decided to test the effect of some efficient inhibitors of DPP-IV on PepX activity ... evolution The existence of the X-PDAP signature led us to test inhibitors of DPP-IV on PepX activity for which no specific inhibitor is known The inhibitors of DPP-IV chosen were those of the smallest...
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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 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 ... proved to be highly useful for the cellular potency screening of PDE1 inhibitors Pretreatment of A cAMP (fold of control) Fig The PDE1 inhibitors compound 31 and compound 30 concentration-dependently...
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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 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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Báo cáo khoa học: Template-assisted rational design of peptide inhibitors of furin using the lysine fragment of the mung bean trypsin inhibitor pptx
... amount of enzyme was added to release 15 nmol of MCA in the enzyme reaction For determination of the inhibitory activity, a fixed amount of enzyme was first incubated with different amounts of the ... disulfide isoforms of this peptide inhibited the enzyme with Ki values of 1.2 · 10-7 m and · 10)8 m [24] A backbone-cyclized, potent trypsin inhibitor, sunflower trypsin inhibitor-1 (SFTI-1), of 14 ... reactive site disulfide loop of nine amino acid residues commonly found in the Bowman–Birk family of inhibitors The disulfide loop in SFTI-1 differs from that in the Lys domain of MBTI by only one noncontact...
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Báo cáo Y học: Synthesis of phosphoenol pyruvate (PEP) analogues and evaluation as inhibitors of PEP-utilizing enzymes pot
... described previously [30] The rate of formation of oxalacetic acid was calculated from the rate of disappearance of NADH Studies were conducted in the presence of 0.3 UÆmL)1 of PEP carboxylase and either ... L-isomer of Ó FEBS 2002 Inhibitors of phosphoenolpyruvate-utilizing enzymes (Eur J Biochem 269) 3233 Fig Lineweaver–Burk plots of inhibition of PEP-utilizing enzymes in the presence of PEP analogs ... screened as inhibitors of (a) enzyme I of the PTS from E coli; (b) rabbit muscle pyruvate kinase; (c) maize PEP carboxylase; and (d) yeast enolase Because the selection of the metal cofactor required...
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Báo cáo khoa học: Alizarine derivatives as new dual inhibitors of the HIV-1 reverse transcriptase-associated DNA polymerase and RNase H activities effective also on the RNase H activity of non-nucleoside resistant reverse transcriptases pot
... HIV-1 RT inhibitors modes of action, we tested a novel series of AQ derivatives based on the alizarine structure and found that some are inhibitors of both RT-associated functions Mode -of- action ... incubated in the presence of different concentrations of K-49 and in the absence () or presence of lM (.) or 10 lM ( ) RDS1643 (B) YonetaniTheorell plot of the interaction of K-49 and efavirenz on ... the presence of different concentrations of efavirenz and in the absence () or presence of 1.9 lM (s), 3.7 lM (.) and 7.5 lM (4) K-49 (C) YonetaniTheorell plot of the interaction of KNA-53 and...
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Báo cáo khoa học: Inhibitors of protein phosphatase 1 and 2A decrease the level of tubulin carboxypeptidase activity associated with microtubules pptx
... value of integrated intensity of Glu-microtubules was divided by that of Tyr-microtubules to estimate the relative proportion of Glu- with respect to Tyr-microtubules Results Exposure of cells ... well-known inhibitors of PP1 and PP2A [23,24], showed effects similar to that of OA (Fig 4) Deltamethrin, a specific inhibitor of PP2B [25], and phenylarsine oxide, a putative inhibitor of tyrosine ... product, detyrosinated tubulin (Glu-tubulin), as a function of incubation time The slope of the time curves provides an estimate of the amount of the associated carboxypeptidase This method showed...
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Báo cáo khoa học: 9-Deazaguanine derivatives connected by a linker to difluoromethylene phosphonic acid are slow-binding picomolar inhibitors of trimeric purine nucleoside phosphorylase potx
... the synthesis of a pro-drug of DFPP-DG to improve its cell penetration The problem of the poor uptake of the compound by cells may, in principle, also be overcome by use of one of the recently ... determination of inhibition constants, and in 50 mm phosphate buffer for determination of the enzyme specic activity One unit of PNP is dened as the amount of enzyme that causes phosphorolysis of lmol of ... of substrate for the active sites of the enzyme; therefore, the slow-onset phase of the reaction may not always be observed [18] This is shown in the left panel of Fig 4, where, in the case of...
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Báo cáo khoa học: Polyphosphates from Mycobacterium bovis – potent inhibitors of class III adenylate cyclases pptx
... of Rv1625c inhibition of combined fractions from the Superose fractionation in (A) 1096 C E B A B Fig 31P-NMR spectra of the concentrated fractions (50–64) of the Superose gel filtration and of ... IC50 of 20 lm, and the cyclic trimetaphosphate an IC50 of mm; that is, these compounds were poor inhibitors (Table 2) In contrast, all IC50 concentrations of poly-Ps with a chain length of 16 ... eight-fold immediately prior to the start of the reaction Reaction velocities of Rv1625c were determined in the presence of 10, 20 and 25 nm polyP75 as a function of the substrate Mn-ATP A Lineweaver–Burk...
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Báo cáo khoa học: Mutant recombinant serpins as highly specific inhibitors of human kallikrein 14 ppt
... dependence of kobs of serpins on hK14 inhibition The association rate constants (ka) were determined from the slope of kobs values versus the concentration of hK14 inhibitors Independent of the inhibitor ... specificity of hK14 inhibitors Inhibition percentage corresponding to 100 *[1–(velocity in presence of inhibitor ⁄ velocity of uninhibited control)] Reaction of 30 incubation with an excess of inhibitor ... (velocity) of hK14 were obtained by adding 20 lM of fluorescent substrate Fractional velocity corresponds to the ratio of the velocity of the inhibited enzyme (vi) to the velocity of the uninhibited...
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Báo cáo Y học: Selection of effective antisense oligodeoxynucleotides with a green fluorescent protein-based assay Discovery of selective and potent inhibitors of glutathione S-transferase Mu expression doc
... effectiveness of a set of antisense PS-ODNs directed against the glutathione S-transferase Mu1 (GSTM1) and Mu2 (GSTM2) isoforms of the rat GSTs play an important role in the detoxification of DNA- and/or ... The number of mismatches in the corresponding region of the nontargeted isoform are given Mismatches are underlined in the sequence Determination of the concentration/activity profile of the AS-ODNs ... another nonspecific inhibitor of EGFP expression as the IC50 values for inhibition of EGFP expression and of EGFP–M1 were both in the same range Analysis of the effect of AS-ODNs on GST activity...
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Henry IV, Makers of History pptx
... Punishment of Coligni. Valor of the survivors. Pledges of aid. Prophecy of Knox. Apology of the court. Opinions of the courts of Europe. Rejoicings at Rome. Atrocity of the deed. Results of the massacre. ... Suspicions of poison. Invectives of the king. Recovery of the king. Disappointment of Francis. Fanaticism of the king. Escape of the Duke of Alençon. The king aroused. War of the public good. Defeat of ... the head of the three rival houses of Valois, of Bourbon, and of Guise One of these was King of France One was King of Navarre But Henry of Guise was, in wealth and in the attachment of the Catholic...
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ultrathin magnetic structures iv. applications of nanomagnetism, 2005, p.269
... have galvanised the efforts of previously disparate research communities by offering the promise of surpassing the limits of conventional semiconductors Clearly the world of magnetism has now entered ... via doping, gate voltages and band offsets Coupling the new degree of freedom of carrier spin with the traditional band gap engineering of modern electronics offers new functionality and performance ... tremendous amount of theoretical and experimental effort addressing the various facets of operation of spin-polarized devices A variety of other semiconductor spintronic devices of varying complexity...
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Báo cáo sinh học: " Peptide inhibitors of dengue virus and West Nile virus infectivity" pot
... infectivity of these viral pathogens of major public health importance The inhibitory effects of these peptides were dose dependent with IC50s in the range of 10 µM Several of the most potent of these ... primary sequence of E1, the fusion protein of Semliki Forest virus, an alphavirus, revealed a remarkable fit to the scaffold of TBEV E [20] suggesting the existence of a second class of viral fusion ... each of the peptides and used to infect monolayers of LLCKM-2 monkey kidney epithelial cells The number of resulting viral foci was determined from three experiments and normalized to a Page of...
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