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[PMID]:28460471
[Au] Autor:Zhao L; Yang G; Bai H; Zhang M; Mou D
[Ad] Endereço:Department of General Surgery, The First Hospital of Tsinghua University, Beijing, China.
[Ti] Título:NCTD promotes Birinapant-mediated anticancer activity in breast cancer cells by downregulation of c-FLIP.
[So] Source:Oncotarget;8(16):26886-26895, 2017 Apr 18.
[Is] ISSN:1949-2553
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Second mitochondria-derived activator of caspases (SMAC) mimetics is a class of new anticancer agents. However, most cancers exhibit de novo or acquired resistance to SMAC mimetics, posting a problem for broad applications in clinic, and highlighting the necessity of exploring combinational strategies to circumvent SMAC mimetic-resistance. We here showed that Norcantharidin, a drug that is currently being used in cancer treatment, significantly enhanced SMAC mimetic Birinapant-mediated cell viability inhibition and robustly promoted apoptosis in established breast carcinoma cell lines, as well as in primary breast carcinoma cells. Mechanistically, we revealed that Norcantharidin effectively reduced the levels of two major protein isoforms of cellular FLICE-like inhibitor protein(c-FLIP), namely c-FLIP long (c-FLIPL) and c-FLIP short (c-FLIPS). Moreover, Norcantharidin markedly enhanced Birinapant-triggered caspase-8/caspase-3 cascade. Inhibition of caspase-8 activity by a synthetic peptide Z-IETD-FMK significantly attenuated cell death induction by the combination, suggesting that caspase-8 plays a critical role in the anticancer action. In conclusion, our study suggests that the combination of SMAC mimetics with Norcantharidin represents a novel strategy in breast cancer therapy and warrants further studies.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Neoplasias da Mama/genética
Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia
Proteína Reguladora de Apoptosis Semelhante a CASP8 e FADD/genética
Dipeptídeos/farmacologia
Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos
Indóis/farmacologia
[Mh] Termos MeSH secundário: Apoptose/efeitos dos fármacos
Caspase 8/metabolismo
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Feminino
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (CASP8 and FADD-Like Apoptosis Regulating Protein); 0 (Dipeptides); 0 (Indoles); 6O4Z07B57R (birinapant); 8452E71EO7 (norcantharidin); EC 3.4.22.- (Caspase 8)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.18632/oncotarget.15848


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[PMID]:29366749
[Au] Autor:Gonzalez EA; Martins GR; Tavares AMV; Viegas M; Poletto E; Giugliani R; Matte U; Baldo G
[Ad] Endereço:Gene Therapy Center, Hospital de Clínicas de Porto Alegre, Porto Alegre, Brazil; Post-Graduation Program in Genetics and Molecular Biology, UFRGS, Porto Alegre, Brazil.
[Ti] Título:Cathepsin B inhibition attenuates cardiovascular pathology in mucopolysaccharidosis I mice.
[So] Source:Life Sci;196:102-109, 2018 Mar 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Mucopolysaccharidosis type I (MPS I) is a lysosomal storage disorder with multisystemic features, including heart enlargement, heart valve dysfunction, and aortic stiffness and dilatation. Previous studies have shown that MPS I mice overexpress cathepsin B (CtsB) in multiple tissues, including those from the cardiovascular system. Here, we hypothesized that inhibition of CtsB could ameliorate cardiac function parameters, as well as aorta and valve abnormalities found in MPS I. First, we found that total elastase activity in an MPS I aorta is elevated. Following that, we demonstrated that CtsB leaks from the lysosome in MPS I human fibroblasts, possibly acting as a degradative agent of extracellular matrix components from the aorta, cardiac muscle, and heart valves. We then used a CtsB inhibitor in vivo in the MPS I mouse model. After 4 months of treatment, partial inhibition of CtsB activity in treated mice reduced aortic dilatation, as well as heart valve thickening, and led to improvements in cardiac function parameters, although none of these were completely normalized. Based on these results, we conclude that lysosomal alterations in this disease promote leakage of CtsB to outside the organelle, where this protein can have multiple pathological roles. CtsB inhibition improved cardiovascular parameters in MPS I mice and can have a potential benefit in this disease.
[Mh] Termos MeSH primário: Sistema Cardiovascular/patologia
Catepsina B/antagonistas & inibidores
Inibidores de Cisteína Proteinase/uso terapêutico
Dipeptídeos/uso terapêutico
Mucopolissacaridose I/diagnóstico por imagem
Mucopolissacaridose I/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Aorta/patologia
Aorta/fisiopatologia
Sistema Cardiovascular/diagnóstico por imagem
Catepsina B/metabolismo
Colagenases/metabolismo
Feminino
Fibroblastos/metabolismo
Testes de Função Cardíaca
Doenças das Valvas Cardíacas/diagnóstico por imagem
Doenças das Valvas Cardíacas/tratamento farmacológico
Doenças das Valvas Cardíacas/patologia
Seres Humanos
Lisossomos/metabolismo
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Mucopolissacaridose I/patologia
Elastase Pancreática/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cysteine Proteinase Inhibitors); 0 (Dipeptides); 134448-10-5 (N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline); EC 3.4.21.36 (Pancreatic Elastase); EC 3.4.22.1 (Cathepsin B); EC 3.4.24.- (Collagenases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180126
[St] Status:MEDLINE


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[PMID]:29340380
[Au] Autor:Fang Z; Wang J; Zhu S; Yang X; Jia Y; Sun Q; Guan S
[Ad] Endereço:School of Materials Science and Engineering, Zhengzhou University, Zhengzhou 450001, China. skguan@zzu.edu.cn.
[Ti] Título:A DFT study of the adsorption of short peptides on Mg and Mg-based alloy surfaces.
[So] Source:Phys Chem Chem Phys;20(5):3602-3607, 2018 Jan 31.
[Is] ISSN:1463-9084
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Adsorption of short peptides, including three dipeptides: arginine-glycine (Arg-Gly), glycine-aspartic acid (Gly-Asp), arginine-aspartic acid (Arg-Asp), and one tripeptide arginine-glycine-aspartic acid (RGD), on the surfaces of Mg and Mg alloys (Mg-Zn, Mg-Y, and Mg-Nd), was studied using the first-principles calculations based on density functional theory (DFT), considering van der Waals (vdW) correction. The calculated adsorption energies (E ) of short peptides on the clean Mg(0001) surface are in the range of -1.73 to -2.80 eV per dipeptide, and -3.24 eV for RGD. The short peptides prefer to bond to Mg atoms at the surface by the O and N anions in their functional groups. For the clean Mg(0001) surface, the E of the short peptides are exclusively dominated by the number of functional groups binding to the surface. However, for the surface of the Mg-Zn alloy (1% Zn), the adsorption of the peptides is clearly enhanced (by about 0.3 eV per peptide) due to the enhanced N-Mg bond and the electrostatic interactions between the doped Zn at the surface and the backbone chains of the peptides. Furthermore, the attractive interactions are increased with the increase of doped Zn contents (up to 3%). In contrast, for the surfaces of Mg-Y (1% Y) and Mg-Nd (1% Nd) alloys, the adsorption of the peptides is slightly weakened compared to that on the clean Mg(0001) surfaces. Our results provide useful guidance in understanding the interactions between peptides and the Mg-based biomedical alloy surfaces at the atomic scale in the biomimetic coating fields.
[Mh] Termos MeSH primário: Ligas/química
Dipeptídeos/química
Magnésio/química
Oligopeptídeos/química
[Mh] Termos MeSH secundário: Adsorção
Dipeptídeos/metabolismo
Oligopeptídeos/metabolismo
Teoria Quântica
Eletricidade Estática
Propriedades de Superfície
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alloys); 0 (Dipeptides); 0 (Oligopeptides); 78VO7F77PN (arginyl-glycyl-aspartic acid); I38ZP9992A (Magnesium)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180118
[St] Status:MEDLINE
[do] DOI:10.1039/c7cp07431j


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[PMID]:29307827
[Au] Autor:Manning ME; Danson EJ; Calderone CT
[Ad] Endereço:Department of Chemistry, Carleton College, 1 North College Street, Northfield, MN 55057, United States.
[Ti] Título:Functional chararacterization of the enzymes TabB and TabD involved in tabtoxin biosynthesis by Pseudomonas syringae.
[So] Source:Biochem Biophys Res Commun;496(1):212-217, 2018 01 29.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Pseudomonas syringae pv. tabaci ATCC 11528 produces tabtoxin, a ß-lactam-containing dipeptide phytotoxin. Tabtoxinine-ß-lactam (TßL), one of tabtoxin's constituent amino acids, structurally mimics lysine, and many of the proteins encoded by the tabtoxin biosynthetic gene cluster are homologs of lysine biosynthetic enzymes, suggesting that the tabtoxin and lysine biosynthetic routes parallel one another. We cloned and expressed TabB and TabD, predicted homologs of tetrahydrodipicolinate (THDPA)-N-acyltransferase and N-acyl-THDPA aminotransferase, respectively, to determine their activities in vitro. We confirmed that TabB succinylates THDPA and that TabD is a PLP-dependent aminotransferase that utilizes glutamate as an amine donor. Surprisingly, we also found that though TabD could utilize the TabB product N-succinyl-THDPA as a substrate, THDPA itself was also recognized. These observations reveal that TabB functionally duplicates DapD, the THDPA-N-succinyltransferase involved in lysine biosynthesis, and reinforce the close relationship between the metabolic logics underpinning the respective biosynthetic pathways.
[Mh] Termos MeSH primário: Acetiltransferases/química
Acetiltransferases/metabolismo
Proteínas de Bactérias/química
Proteínas de Bactérias/metabolismo
Dipeptídeos/biossíntese
Pseudomonas syringae/metabolismo
Transaminases/química
Transaminases/metabolismo
[Mh] Termos MeSH secundário: Ativação Enzimática
Estabilidade Enzimática
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Bacterial Proteins); 0 (Dipeptides); EC 2.3.1.- (Acetyltransferases); EC 2.3.1.- (TabB protein, Pseudomonas syringae); EC 2.6.1.- (Transaminases); H3YX70R64N (tabtoxin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180215
[Lr] Data última revisão:
180215
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180109
[St] Status:MEDLINE


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[PMID]:29294327
[Au] Autor:Ren C; Liu J; Zhou J; Liang H; Wang Y; Sun Y; Ma B; Yin Y
[Ad] Endereço:Departments of Human Anatomy, Histology and Embryology, Peking University Health Science Center, Beijing 100191, China.
[Ti] Título:Low levels of serum serotonin and amino acids identified in migraine patients.
[So] Source:Biochem Biophys Res Commun;496(2):267-273, 2018 02 05.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Migraine is a highly disabling primary headache associated with a high socioeconomic burden and a generally high prevalence. The clinical management of migraine remains a challenge. This study was undertaken to identify potential serum biomarkers of migraine. Using Liquid Chromatography coupled to Mass Spectrometry (LC-MS), the metabolomic profile of migraine was compared with healthy individuals. Principal component analysis (PCA) and Orthogonal partial least squares-discriminant analysis (orthoPLS-DA) showed the metabolomic profile of migraine is distinguishable from controls. Volcano plot analysis identified 10 serum metabolites significantly decreased during migraine. One of these was serotonin, and the other 9 were amino acids. Pathway analysis and enrichment analysis showed tryptophan metabolism (serotonin metabolism), arginine and proline metabolism, and aminoacyl-tRNA biosynthesis are the three most prominently altered pathways in migraine. ROC curve analysis indicated Glycyl-l-proline, N-Methyl-dl-Alanine and l-Methionine are potential sensitive and specific biomarkers for migraine. Our results show Glycyl-l-proline, N-Methyl-dl-Alanine and l-Methionine may be as specific or more specific for migraine than serotonin which is the traditional biomarker of migraine. We propose that therapeutic manipulation of these metabolites or metabolic pathways may be helpful in the prevention and treatment of migraine.
[Mh] Termos MeSH primário: Alanina/análogos & derivados
Dipeptídeos/sangue
Metionina/sangue
Transtornos de Enxaqueca/diagnóstico
Serotonina/sangue
[Mh] Termos MeSH secundário: Adulto
Alanina/sangue
Arginina/sangue
Biomarcadores/sangue
Estudos de Casos e Controles
Cromatografia Líquida de Alta Pressão/métodos
Análise Discriminante
Feminino
Seres Humanos
Masculino
Metaboloma
Transtornos de Enxaqueca/sangue
Transtornos de Enxaqueca/fisiopatologia
Análise de Componente Principal
Prolina/sangue
Aminoacil-RNA de Transferência/sangue
Curva ROC
Triptofano/sangue
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Biomarkers); 0 (Dipeptides); 0 (RNA, Transfer, Amino Acyl); 333DO1RDJY (Serotonin); 600-21-5 (N-methylalanine); 704-15-4 (glycylproline); 8DUH1N11BX (Tryptophan); 94ZLA3W45F (Arginine); 9DLQ4CIU6V (Proline); AE28F7PNPL (Methionine); OF5P57N2ZX (Alanine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180214
[Lr] Data última revisão:
180214
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180103
[St] Status:MEDLINE


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[PMID]:29253571
[Au] Autor:Nasrin A; Hassan M; Ye P
[Ad] Endereço:Faculty of Dentistry, The University of Sydney, Sydney, Australia.
[Ti] Título:Inhibition of Notch signaling pathway using γ-secretase inhibitor delivered by a low dose of Triton-X100 in cultured oral cancer cells.
[So] Source:Biochem Biophys Res Commun;495(3):2118-2124, 2018 01 15.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:How to effectively delivering therapeutic agents, including γ-secretase inhibitors (GSIs), into live cells, remains a significant challenge. This study assessed the effect of Notch signaling inhibition by examining levels of the Notch1 intracellular domain (N1ICD) in cultured oral cancer cells analyzed with random stitched images (2D) and 3D visualizations using confocal microscopy and quantitative gene analysis. Substantially, we have developed a novel method to assist the delivery of γ-secretase inhibitor, DAPT, into live cells in the presence of an effective minimum concentration of Triton-X100 (0.001%) without damaging cell activity and membrane integrity assessed with cell proliferation assays. The images obtained in this study showed that DAPT alone could not block the γ-secretase inhibitor despite inhibiting cell growth. Further analysis of quantitative gene expressions of Notch signaling canonical pathway to verify the effectiveness of the novel method for delivering inhibitor into live cells, displayed deregulation of Notch1, Delta-like ligand 1 (DLL1) and hairy and enhancer of split 1 (Hes1). Our data suggest that Notch1/Hes1 signaling pathway is deactivated using DAPT with a low dose of Triton-X100 in this cancer cells. And the finding also suggests that Notch1 could be engaged by DLL1 to promote differentiation in oral cancer cells. Using this approach, we demonstrate that Triton-X100 is a promising and effective permeabilization agent to deliver γ-secretase inhibitor DAPT into live oral epithelial cells. This strategy has the potential to implicate in the treatment of cancer diseases.
[Mh] Termos MeSH primário: Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores
Dipeptídeos/administração & dosagem
Neoplasias Bucais/tratamento farmacológico
Neoplasias Bucais/metabolismo
Octoxinol/administração & dosagem
Receptor Notch1/metabolismo
Transdução de Sinais/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antineoplásicos/administração & dosagem
Antineoplásicos/química
Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Dipeptídeos/farmacologia
Relação Dose-Resposta a Droga
Sinergismo Farmacológico
Emulsões/química
Seres Humanos
Neoplasias Bucais/patologia
Octoxinol/química
Octoxinol/farmacologia
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Dipeptides); 0 (Emulsions); 0 (N-(N-(3,5-difluorophenacetyl)alanyl)phenylglycine tert-butyl ester); 0 (NOTCH1 protein, human); 0 (Receptor, Notch1); 9002-93-1 (Octoxynol); EC 3.4.- (Amyloid Precursor Protein Secretases)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180213
[Lr] Data última revisão:
180213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171219
[St] Status:MEDLINE


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[PMID]:29282980
[Au] Autor:Wu GC; Lin SY; Liang HJ; Hou WC
[Ti] Título:135-Day Interventions of Yam Dioscorin and the Dipeptide Asn-Trp (NW) To Reduce Weight Gains and Improve Impaired Glucose Tolerances in High-Fat Diet-Induced C57BL/6 Mice.
[So] Source:J Agric Food Chem;66(3):645-652, 2018 Jan 24.
[Is] ISSN:1520-5118
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The C57BL/6J mice were fed a 135-day normal diet or a high-fat diet (HFD) without, or concurrent with, a single yam dioscorin (80 mg/kg) or dipeptide NW (40 mg/kg) intervention every day. The final body weights (g) of mice were 26.1 ± 1.4, 34.97 ± 2.1, 31.75 ± 2.6, and 31.66 ± 3.1, respectively, for normal diet-fed, HFD-fed, dioscorin-intervened, and NW-intervened group. The mice in both intervened groups showed similar less weight gains and had significant differences (P < 0.05) compared to those in the HFD group under the same cumulative HFD intakes. The blood biochemical index of mice with dioscorin interventions showed significantly lower contents in total cholesterol and low-density lipoprotein, and NW interventions showed significantly lower total triglyceride contents compared to those of the HFD group (P < 0.05). Both intervened mice exhibited similar reductions in total visceral lipid contents and have significant differences compared to those of the HFD group (P < 0.05). The dioscorin intervention was better than NW interventions in lowering blood glucose levels by oral glucose tolerance tests and both showed significant differences (P < 0.05) compared to those in the HFD group. Yam dioscorin or dipeptide NW will potentially be used for preventive functional foods of less body weight gains and impaired glucose tolerance controls, which require further clinical trial investigations.
[Mh] Termos MeSH primário: Dioscorea/química
Dipeptídeos/administração & dosagem
Obesidade/tratamento farmacológico
Proteínas de Plantas/química
[Mh] Termos MeSH secundário: Animais
Glicemia/metabolismo
Dieta Hiperlipídica/efeitos adversos
Dipeptídeos/química
Intolerância à Glucose
Seres Humanos
Lipoproteínas LDL/sangue
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Obesidade/metabolismo
Obesidade/fisiopatologia
Proteínas de Plantas/administração & dosagem
Triglicerídeos/sangue
Ganho de Peso/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Blood Glucose); 0 (Dipeptides); 0 (Lipoproteins, LDL); 0 (Plant Proteins); 0 (Triglycerides); 0 (dioscorin protein, Dioscorea)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180207
[Lr] Data última revisão:
180207
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171229
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jafc.7b05564


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[PMID]:29183661
[Au] Autor:El-Wahab HAAA; Accietto M; Marino LB; McLean KJ; Levy CW; Abdel-Rahman HM; El-Gendy MA; Munro AW; Aboraia AS; Simons C
[Ad] Endereço:School of Pharmacy and Pharmaceutical Sciences, Cardiff University, Cardiff CF10 3NB, Wales, UK; Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt.
[Ti] Título:Design, synthesis and evaluation against Mycobacterium tuberculosis of azole piperazine derivatives as dicyclotyrosine (cYY) mimics.
[So] Source:Bioorg Med Chem;26(1):161-176, 2018 01 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Three series of azole piperazine derivatives that mimic dicyclotyrosine (cYY), the natural substrate of the essential Mycobacterium tuberculosis cytochrome P450 CYP121A1, were prepared and evaluated for binding affinity and inhibitory activity (MIC) against M. tuberculosis. Series A replaces one phenol group of cYY with a C3-imidazole moiety, series B includes a keto group on the hydrocarbon chain preceding the series A imidazole, whilst series C explores replacing the keto group of the piperidone ring of cYY with a CH -imidazole or CH -triazole moiety to enhance binding interaction with the heme of CYP121A1. The series displayed moderate to weak type II binding affinity for CYP121A1, with the exception of series B 10a, which displayed mixed type I binding. Of the three series, series C imidazole derivatives showed the best, although modest, inhibitory activity against M. tuberculosis (17d MIC = 12.5 µg/mL, 17a 50 µg/mL). Crystal structures were determined for CYP121A1 bound to series A compounds 6a and 6b that show the imidazole groups positioned directly above the haem iron with binding between the haem iron and imidazole nitrogen of both compounds at a distance of 2.2 Å. A model generated from a 1.5 Šcrystal structure of CYP121A1 in complex with compound 10a showed different binding modes in agreement with the heterogeneous binding observed. Although the crystal structures of 6a and 6b would indicate binding with CYP121A1, the binding assays themselves did not allow confirmation of CYP121A1 as the target.
[Mh] Termos MeSH primário: Antituberculosos/farmacologia
Azóis/farmacologia
Dipeptídeos/farmacologia
Desenho de Drogas
Mycobacterium tuberculosis/efeitos dos fármacos
Peptídeos Cíclicos/farmacologia
Piperazinas/farmacologia
[Mh] Termos MeSH secundário: Antituberculosos/síntese química
Antituberculosos/química
Azóis/química
Sítios de Ligação/efeitos dos fármacos
Sistema Enzimático do Citocromo P-450/química
Sistema Enzimático do Citocromo P-450/metabolismo
Dipeptídeos/química
Relação Dose-Resposta a Droga
Ligantes
Testes de Sensibilidade Microbiana
Modelos Moleculares
Estrutura Molecular
Mycobacterium tuberculosis/metabolismo
Peptídeos Cíclicos/química
Piperazinas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antitubercular Agents); 0 (Azoles); 0 (Dipeptides); 0 (Ligands); 0 (Peptides, Cyclic); 0 (Piperazines); 0 (cytochrome P-450 CYP12A1 (house fly)); 1RTM4PAL0V (piperazine); 5625-40-1 (cyclo(tyrosyl-tyrosyl)); 9035-51-2 (Cytochrome P-450 Enzyme System)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180106
[Lr] Data última revisão:
180106
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171130
[St] Status:MEDLINE


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[PMID]:28460361
[Au] Autor:Zivkovic MD; Rajkovic S; Glisic BD; Draskovic NS; Djuran MI
[Ad] Endereço:University of Kragujevac, Faculty of Science, Department of Chemistry, Radoja Domanovica 12, 34000 Kragujevac, Serbia. Electronic address: mzivkovic@kg.ac.rs.
[Ti] Título:Hydrolysis of the amide bond in histidine- and methionine-containing dipeptides promoted by pyrazine and pyridazine palladium(II)-aqua dimers: Comparative study with platinum(II) analogues.
[So] Source:Bioorg Chem;72:190-198, 2017 06.
[Is] ISSN:1090-2120
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Two dinuclear palladium(II) complexes, [{Pd(en)Cl} (µ-pz)](NO ) and [{Pd(en)Cl} (µ-pydz)](NO ) , have been synthesized and characterized by elemental microanalysis and spectroscopic ( H and C NMR, IR and UV-vis) techniques (en is ethylenediamine; pz is pyrazine and pydz is pyridazine). The square planar geometry of palladium(II) metal centers in these complexes has been predicted by DFT calculations. The chlorido complexes were converted into the corresponding aqua complexes, [{Pd(en)(H O)} (µ-pz)] and [{Pd(en)(H O)} (µ-pydz)] , and their reactions with N-acetylated l-histidylglycine (Ac-l-His-Gly) and l-methionylglycine (Ac-l-Met-Gly) were studied by H NMR spectroscopy. The palladium(II)-aqua complexes and dipeptides were reacted in 1:1 M ratio, and all reactions performed in the pH range 2.0
[Mh] Termos MeSH primário: Amidas/química
Dipeptídeos/química
Histidina/química
Metionina/química
Compostos Organometálicos/química
[Mh] Termos MeSH secundário: Dimerização
Relação Dose-Resposta a Droga
Hidrólise
Estrutura Molecular
Paládio/química
Platina/química
Pirazinas/química
Piridazinas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amides); 0 (Dipeptides); 0 (Organometallic Compounds); 0 (Pyrazines); 0 (Pyridazines); 49DFR088MY (Platinum); 4QD397987E (Histidine); 5TWQ1V240M (Palladium); AE28F7PNPL (Methionine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171214
[Lr] Data última revisão:
171214
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170502
[St] Status:MEDLINE


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[PMID]:28873586
[Au] Autor:Wang L; Ding Y; Zhang X; Li Y; Wang R; Luo X; Li Y; Li J; Chen Z
[Ad] Endereço:State Key Laboratory of Food Science and Technology, Jiangnan University, Lihu Road 1800, Wuxi 214122, China; School of Food Science and Technology, National Engineering Laboratory for Cereal Fermentation Technology, Jiangnan University, Lihu Road 1800, Wuxi 214122, China. Electronic address: legend
[Ti] Título:Isolation of a novel calcium-binding peptide from wheat germ protein hydrolysates and the prediction for its mechanism of combination.
[So] Source:Food Chem;239:416-426, 2018 Jan 15.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:To isolate a novel peptide with specific calcium-binding capacity, wheat germ protein was hydrolyzed. The hydrolysates were purified using ultrafiltration, anion-exchange chromatography, gel filtration chromatography, and reversed-phase high performance liquid chromatography. The amino acid sequence of the purified peptide was determined and confirmed to be FVDVT (Phe-Val-Asp-Val-Thr). The calcium-binding capacity of FVDVT reached 89.94±0.75%, increased by 86.37% compared to the hydrolysates. The chelating mechanism between FVDVT and calcium was further investigated by Ultraviolet-Visible absorption spectroscopy, Fourier transform infrared spectroscopy, X-ray diffraction, and H nuclear magnetic resonances spectroscopy. The results indicated that the oxygen atoms of the carboxy group and the nitrogen atoms of the amido group provided major binding sites. In addition, aspartic acid and threonine show considerable capacity for incorporating with calcium by donating electron pairs. This study provides a feasible approach to isolate calcium-binding peptides and to clarify the possible binding mechanism of calcium and peptide.
[Mh] Termos MeSH primário: Triticum
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Cálcio
Dipeptídeos
Peptídeos
Hidrolisados de Proteína
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dipeptides); 0 (Peptides); 0 (Protein Hydrolysates); 0 (phenylalanyl-valine); SY7Q814VUP (Calcium)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171128
[Lr] Data última revisão:
171128
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170907
[St] Status:MEDLINE



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