Synthesis of guanidino analogues as potential nitric oxide synthase inhibitors
Synthesis of guanidino analogues as potential nitric oxide synthase inhibitors
... SYNTHESIS OF GUANIDINO ANALOGUES AS POTENTIAL NITRIC OXIDE SYNTHASE INHIBITORS BONG YONG KOY 2004 SYNTHESIS OF GUANIDINO ANALOGUES AS POTENTIAL NITRIC OXIDE SYNTHASE INHIBITORS BONG ... Oxide Synthase (NOS) Isoforms of Nitric Oxide Synthase Physiological Roles of NO and Pathology of NO Overproduction Inhibition of Nitric Oxide Synthase X-Ray Crystallographic Structure of NOS ... List of Figures xiii List of Schemes xiv List of Tables xv Chapter 1 Nitric Oxide and Nitric Oxide Synthase Nitric Oxide (NO): Properties and Biological Effects In vivo NO Production: Nitric Oxide...
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Nitroguanidines and guanidino containing hetereocycles as potential nitric oxide synthase inhibitors
... Chemistry of Nitric Oxide 1.2 Nitric Oxide and Nitric Oxide Synthase 1.3 Nitric Oxide Synthase Isoforms 1.4 NOS Structure and Function 10 1.4.1 NADPH and Oxygen 11 1.4.2 Calmodulin 12 1.4.3 FAD and FMN ... Whereas for the inducible mode, NO is generated in large fluxes and is associated with the destructive indirect biological effects of NO.[3, 20] 1.2 Nitric Oxide and Nitric Oxide Synthase NO has ... cardiovascular, neuronal, and immune systems The overproduction of NO by nitric oxide synthase (NOS) has been implicated in many diseases therefore inhibitors of NOS may be useful as therapeutic agents...
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Báo cáo khoa học: "Immunohistochemical study of constitutive neuronal and inducible nitric oxide synthase in the central nervous system of goat with natural listeriosis" potx
... counterstained with hematoxylin Magnification A and B, ×66 C and D, ×132 Immunohistochmical study of nitric oxide synthase in the central nervous system of goat Enhanced expression of nNOS and iNOS in ... is the first study of NOS expression in the goat brain with listeriosis The involvement of iNOS in bovine and caprine listeriosis has been reported previously, and the increased expression of iNOS ... microabscesses, and some astrocytes (identical in Fig Histology and immunostaining of caprine brains with natural listeriosis A: Brain of a goat with listeriosis showing meningoencephalitis H-E staining,...
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Báo cáo y học: "Characterization of Human Erythrocytes as Potential Carrier for Pravastatin: An In Vitro Study"
... of pravastatin in human erythrocytes The current work studies effect of time, temperature as well as drug concentration on the process of pravastatin loading into human erythrocytes by endocytosis ... characterization of pravastatin loaded erythrocytes Hematological Indices To determine the effect of loading process on erythrocytes, normal erythrocytes, erythrocytes suspended in PBS, and pravastatin-loaded ... Koitabashi Y, Kumai T, Matsumoto N, Watanabe M, Sekine S, Yanagida Y, Kobayashi S Orange juice increased the bioavailability of pravastatin, 3-hydroxy-3-methylglutaryl CoA reductase inhibitor, in...
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Tài liệu Báo cáo khoa học: Structural and mechanistic aspects of flavoproteins: electron transfer through the nitric oxide synthase flavoprotein domain pdf
... the rate of electron import into the FMN subdomain and the resulting formation of FMNH2 The extent to which KeqA or the rate of FMNH2 formation influences electron flux through the NOS flavoprotein ... NOS, the second electron is provided to the hemedioxy species by a bound H4B cofactor rather than by the flavoprotein domain [16] The H4B radical is then reduced within the enzyme by the flavoprotein ... incomplete extents as the flavoprotein cycles through its 3- and 2 -electron reduced states during catalysis This, in turn, can impact the rate of electron exit and flux through the flavoprotein Two studies...
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Tài liệu Báo cáo khoa học: Polarized distribution of inducible nitric oxide synthase regulates activity in intestinal epithelial cells pdf
... localization of iNOS to apical domains of intestinal epithelial cells Particulate fraction association of iNOS in vivo In order to determine the distribution of iNOS in intestinal epithelial cells in vivo, ... epithelial cells Apical distribution of iNOS in intestinal epithelial cells To get more insight into the localization of iNOS in intestinal cells, Caco-2 cells were investigated Caco-2 FEBS Journal ... which, in intestinal cells, could be bacteria present in the intestinal lumen This hypothesis is supported by positioning of iNOS on the apical side of intestinal crypts Recently PDZ-binding a2...
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Báo cáo khoa học: Binding and activation of nitric oxide synthase isozymes by calmodulin EF hand pairs potx
... isoforms of NOS with CaM-TnC chimeras demonstrated that the roles of the four EF hands in the binding and activation of the cNOS and iNOS enzymes are distinct [13] Replacement of any CaM EF hand ... enzymes during binding and activation [4,5] The present investigation, designed to further assess the role of the two CaM EF hand pairs in the binding and activation of nitric oxide synthase (NOS; EC ... of the target peptide with EF hand in closest contact with the reductase domains The central helix is composed of the C-terminal and N-terminal helices of EF hand units and 3, respectively, and...
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Báo cáo khoa học: Relationship between the structure of guanidines and N-hydroxyguanidines, their binding to inducible nitric oxide synthase (iNOS) and their iNOS-catalysed oxidation to NO pptx
... related to the binding of l-Arg [10–14] and NOHA [10], nothing is known about the thermodynamics and kinetics of the binding of guanidines and N-hydroxyguanidines to iNOS Removal of the a-amino or ... from the conversion of the LS NOS–Fe(III)–ImH complex to the HS NOS–Fe(III)–l-Arg complex was observed Inhibition of the binding of l-Arg to iNOSoxy by ImH, and of the iNOS-catalysed conversion of ... BuNOHG to iNOS is favoured slightly over its binding to nNOS The Km value for the oxidation of BuNOHG by iNOS and nNOS were also found to follow the order iNOS < nNOS [4,6,9] It appears that the...
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Báo cáo khoa học: Rapamycin inhibits lipopolysaccharide induction of granulocyte-colony stimulating factor and inducible nitric oxide synthase expression in macrophages by reducing the levels of octamer-binding factor-2 doc
... octamer and the factors binding to it in LPS-induced gene expression Although involvement of octamer-binding factor- 1 (Oct-1), another octamer-binding protein, cannot be excluded in the LPSinduced expression ... expression of iNOS and G-CSF protein and mRNA were evaluated in macrophages, and the involvement of Oct-2 in LPS ⁄ mTOR-induced iNOS and G-CSF expression was investigated further Results Rapamycin inhibits ... and be inhibited by the mTOR inhibitor, rapamycin In addition, Oct-2 is involved in the expression of LPS -inducible genes that contain octamer in their promoters [24,25] Thus, rapamycin may inhibit...
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Báo cáo khoa học: Proteolytic degradation of nitric oxide synthase isoforms by calpain is modulated by the expression levels of HSP90 potx
... Ca2+ Degradation of NOS isozymes by calpain binding capacity of calpain The physiological relevance of this novel property of HSP90 is also discussed Results Degradation of NOS isozymes in Ca2+ ... intracellular localization of the synthase Degradation of NOS isozymes by calpain The physiological relevance of these findings becomes particularly evident on the basis of the results observed in ... Involvement of the proteasome in activation of endothelial nitric oxide synthase Life Sci 73, 2225–2236 Musial A & Eissa T (2001) Inducible nitric- oxide synthase is regulated by the proteasome degradation...
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Báo cáo khoa học: Cupiennin 1a, an antimicrobial peptide from the venom of the neotropical wandering spider Cupiennius salei, also inhibits the formation of nitric oxide by neuronal nitric oxide synthase pptx
... hydrophobic anchors Given the length of the first helix of cupiennin 1a, and the number of hydrophobic anchors available, it seems likely that the cupiennin 1a ⁄ Ca2+-CaM complex is analogous to the structure ... that cupiennin 1a also complexes with Ca2+-CaM, and is one of the more active of the known peptide inhibitors of nNOS Cupiennin 1a from Cupiennius salei Results Cupiennin 1a was tested for the ... this peptide showed some structural features in common with certain amphibian peptides that inhibit the formation of NO by neuronal nitric oxide synthase (nNOS) [10] These particular amphibian peptides...
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Báo cáo khoa học: In vivo degradation of nitric oxide synthase (NOS) and heat shock protein 90 (HSP90) by calpain is modulated by the formation of a NOS–HSP90 heterocomplex pot
... In vivo degradation of NOS and HSP90 by calpain M Averna et al Table Levels of native and 15 kDa calpastatin species in brain and aorta of NMS and HMS rats treated with HSD for weeks The data ... compilation ª 2008 FEBS M Averna et al In vivo degradation of NOS and HSP90 by calpain higher than in aorta, resulting in a much higher HSP90 to NOS ratio in brain (Fig 1C) A Calpain activation in ... inactivated As both the inactivation and fragmentation of calpastatin are known to be produced by active calpain [32], these observations further indicate that calpain is activated in both tissues, although...
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Báo cáo khoa học: Thermodynamic and kinetic analysis of the isolated FAD domain of rat neuronal nitric oxide synthase altered in the region of the FAD shielding residue Phe1395 docx
... tryptophan in the isolated FAD domain of rat nNOS (F1395W, F1395S and F1395A) and by probing the thermodynamic and kinetic consequences of these mutations We have studied the thermodynamic and kinetic ... determination of the midpoint reduction potentials of flavin cofactors, and also of the haems in the case of NOS and P450 BM3 In spectroelectrochemical titrations of the isolated domains, the lack of ... Fig The coenzyme-binding site in nNOS FAD domain and sequence alignments around the conserved aromatic residue in this domain (A) The nicotinamide-binding site of nNOS FAD domain showing the...
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Báo cáo Y học: Amphibian peptides that inhibit neuronal nitric oxide synthase The isolation of lesueurin from the skin secretion of the Australian Stony Creek Frog Litoria lesueuri docx
... antimicrobial peptides, unlike the majority of the other members of the genus Litoria Instead, it produces a neuropeptide that inhibits the formation of nitric oxide by neuronal nitric oxide synthase ... bioactivity The peptides that inhibit the formation of nitric oxide from nNOS either play a role in the fundamental physiology of the animal, and/or are part of the defence arsenal to combat attack by ... two bioactive peptides from the skin glands of the stony creek frog Litoria lesueuri We have not studied a member of the L lesueuri complex of frogs previously, and we have now found that it does...
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báo cáo hóa học: " Signaling pathways mediating a selective induction of nitric oxide synthase II by tumor necrosis factor alpha in nerve growth factor-responsive cells" pptx
... in the human brain after fatal head injury J Neurotrauma 2002, 19:279-84 Macdonald NJ, Taglialatela G: Tumor necrosis factor alpha and nerve growth factor synergistically induce iNOS in pheochromocytoma ... Cuzzocrea S: Inhibition of the nuclear factor- kappaB activation with pyrrolidine dithiocarbamate attenuating inflammation and oxidative stress after experimental spinal cord trauma in rats J Neurosurg ... example, inflammatory involvement in AD pathogenesis has been proposed partly based on observations of increased levels of the pro-inflammatory cytokines tumor necrosis factor alpha (TNFα) and...
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Từ khóa: transition state analogues of enzymatic reaction as potential drugsdosage as reported by patients and their partners figure 58 mechanism of action of sildenafil viagra® nitric oxide no is produced by the enzyme nitric oxide synthase nos found inthe design and development of imidazothiazolechalcone derivatives as potential anticancer drugsregulation of nitric oxide synthasenitric oxide synthase independent actions of methylargininescarboxyl terminal pdz ligand of neuronal nitric oxide synthasetherapeutic effects of nitric oxide synthase inhibition in neuronal injuryjh lim hj lee hj kim hd jeon r ryu jh 2008 quot inhibition of lipopolysaccharide induced inducible nitric oxide synthase and cyclooxygenase 2 expression by xanthanolides isolated from xanthium strumarium quot bioorg med chem lett 18 6 pp 2179 82functionalization of curcumin analogues as wnt antagonists in osteosarcomaimmunological nitric oxide synthase inos1 17 antibodies attenuates neuronal nitric oxide synthase up regulation edema formation and cell injury following focal trauma to the rat spinal cord pdfnitric oxide and inducible nitric oxide synthasereceptor atrial natriuretic peptide nitric oxide synthase and estrogen receptor mrnas expression in ratnitric oxide synthase in retinal vascular diseasesca2 independent nitric oxide synthase activation in endothelial cellsNghiên cứu sự biến đổi một số cytokin ở bệnh nhân xơ cứng bì hệ thốngNghiên cứu sự hình thành lớp bảo vệ và khả năng chống ăn mòn của thép bền thời tiết trong điều kiện khí hậu nhiệt đới việt namNghiên cứu tổ chức pha chế, đánh giá chất lượng thuốc tiêm truyền trong điều kiện dã ngoạiNghiên cứu tổ hợp chất chỉ điểm sinh học vWF, VCAM 1, MCP 1, d dimer trong chẩn đoán và tiên lượng nhồi máu não cấpGiáo án Sinh học 11 bài 13: Thực hành phát hiện diệp lục và carôtenôitĐỒ ÁN NGHIÊN CỨU CÔNG NGHỆ KẾT NỐI VÔ TUYẾN CỰ LY XA, CÔNG SUẤT THẤP LPWANQuản lý hoạt động học tập của học sinh theo hướng phát triển kỹ năng học tập hợp tác tại các trường phổ thông dân tộc bán trú huyện ba chẽ, tỉnh quảng ninhPhối hợp giữa phòng văn hóa và thông tin với phòng giáo dục và đào tạo trong việc tuyên truyền, giáo dục, vận động xây dựng nông thôn mới huyện thanh thủy, tỉnh phú thọPhát hiện xâm nhập dựa trên thuật toán k meansĐịnh tội danh từ thực tiễn huyện Cần Giuộc, tỉnh Long An (Luận văn thạc sĩ)Tìm hiểu công cụ đánh giá hệ thống đảm bảo an toàn hệ thống thông tinChuong 2 nhận dạng rui roTranh tụng tại phiên tòa hình sự sơ thẩm theo pháp luật tố tụng hình sự Việt Nam từ thực tiễn xét xử của các Tòa án quân sự Quân khu (Luận văn thạc sĩ)Giáo án Sinh học 11 bài 14: Thực hành phát hiện hô hấp ở thực vậtGiáo án Sinh học 11 bài 14: Thực hành phát hiện hô hấp ở thực vậtGiáo án Sinh học 11 bài 14: Thực hành phát hiện hô hấp ở thực vậtBÀI HOÀN CHỈNH TỔNG QUAN VỀ MẠNG XÃ HỘIChiến lược marketing tại ngân hàng Agribank chi nhánh Sài Gòn từ 2013-2015MÔN TRUYỀN THÔNG MARKETING TÍCH HỢPQUẢN LÝ VÀ TÁI CHẾ NHỰA Ở HOA KỲ