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[PMID]:29280407
[Au] Autor:Angeli A; Chiaramonte N; Manetti D; Romanelli MN; Supuran CT
[Ad] Endereço:a Dipartimento Neurofarba , Università degli Studi di Firenze, Sezione di Scienze Farmaceutiche e Nutraceutiche , Sesto Fiorentino (Florence) , Italy.
[Ti] Título:Investigation of piperazines as human carbonic anhydrase I, II, IV and VII activators.
[So] Source:J Enzyme Inhib Med Chem;33(1):303-308, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Four human (h) carbonic anhydrase isoforms (CA, EC 4.2.1.1), hCA I, II, IV, and VII, were investigated for their activation profile with piperazines belonging to various classes, such as N-aryl-, N-alkyl-, N-acyl-piperazines as well as 2,4-disubstituted derivatives. As the activation mechanism involves participation of the activator in the proton shuttling between the zinc-coordinated water molecule and the external milieu, these derivatives possessing diverse basicity and different scaffolds were appropriate for being investigated as CA activators (CAAs). Most of these derivatives showed CA activating properties against hCA I, II, and VII (cytosolic isoforms) but were devoid of activity against the membrane-associated hCA IV. For hCA I, the K s were in the range of 32.6-131 µM; for hCA II of 16.2-116 µM, and for hCA VII of 17.1-131 µM. The structure-activity relationship was intricate and not easy to rationalize, but the most effective activators were 1-(2-piperidinyl)-piperazine (K of 16.2 µM for hCA II), 2-benzyl-piperazine (K of 17.1 µM for hCA VII), and 1-(3-benzylpiperazin-1-yl)propan-1-one (K of 32.6 µM for hCA I). As CAAs may have interesting pharmacologic applications in cognition and for artificial tissue engineering, investigation of new classes of activators may be crucial for this relatively new research field.
[Mh] Termos MeSH primário: Anidrase Carbônica II/antagonistas & inibidores
Anidrase Carbônica IV/antagonistas & inibidores
Anidrase Carbônica I/antagonistas & inibidores
Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
Piperazinas/farmacologia
[Mh] Termos MeSH secundário: Anidrase Carbônica I/metabolismo
Anidrase Carbônica II/metabolismo
Anidrase Carbônica IV/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Relação Dose-Resposta a Droga
Seres Humanos
Modelos Moleculares
Estrutura Molecular
Piperazinas/síntese química
Piperazinas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Piperazines); EC 4.2.1.- (Carbonic Anhydrase I); EC 4.2.1.- (Carbonic Anhydrase II); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (CA4 protein, human); EC 4.2.1.1 (Carbonic Anhydrases); EC 4.2.1.1 (carbonic anhydrase VI)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180105
[Lr] Data última revisão:
180105
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171228
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1417277


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[PMID]:28891338
[Au] Autor:Kumar R; Sharma V; Bua S; Supuran CT; Sharma PK
[Ad] Endereço:a Department of Chemistry , Kurukshetra University , Kurukshetra , India.
[Ti] Título:Synthesis and biological evaluation of benzenesulphonamide-bearing 1,4,5-trisubstituted-1,2,3-triazoles possessing human carbonic anhydrase I, II, IV, and IX inhibitory activity.
[So] Source:J Enzyme Inhib Med Chem;32(1):1187-1194, 2017 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A library of benzenesulphonamides incorporating 1,2,3-triazole rings functionalised with ester, carboxylic acid, carboxamide, carboxyhydrazide, and hydroxymethyl moieties were synthesised. The carbonic anhydrase (CAs, EC 4.2.1.1) inhibitory activity of the new compounds was assessed against four human (h) isoforms, hCA I, hCA II, hCA IV, and hCA IX. Among them, hCA II and IV are anti-glaucoma drug targets, being involved in aqueous humour secretion within the eye. hCA I was inhibited with Ki's ranging between 8.3 nM and 0.8737 µM. hCA II, the physiologically dominant cytosolic isoform, was excellently inhibited by these compounds, with Ki's in the range of 1.6-9.4 nM, whereas hCA IV was effectively inhibited by most of them, with Ki's in the range of 1.4-55.3 nM. Thirteen of the twenty sulphonamides were found to be excellent inhibitors of tumour associated hCA IX with Ki's ≤ 9.5 nM. Many of the new compounds reported here showed low nM inhibitory action against hCA II, IV, and IX, isoforms involved in glaucoma and some tumours, making them interesting candidates for further medicinal chemistry/pharmacologic studies.
[Mh] Termos MeSH primário: Inibidores da Anidrase Carbônica/farmacologia
Sulfonamidas/farmacologia
Triazóis/farmacologia
[Mh] Termos MeSH secundário: Anidrase Carbônica I/antagonistas & inibidores
Anidrase Carbônica I/metabolismo
Anidrase Carbônica II/antagonistas & inibidores
Anidrase Carbônica II/metabolismo
Anidrase Carbônica IV/antagonistas & inibidores
Anidrase Carbônica IV/metabolismo
Anidrase Carbônica IX/antagonistas & inibidores
Anidrase Carbônica IX/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Relação Dose-Resposta a Droga
Seres Humanos
Estrutura Molecular
Relação Estrutura-Atividade
Sulfonamidas/síntese química
Sulfonamidas/química
Triazóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Sulfonamides); 0 (Triazoles); 98-10-2 (benzenesulfonamide); EC 4.2.1.- (Carbonic Anhydrase I); EC 4.2.1.- (Carbonic Anhydrase II); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (Carbonic Anhydrase IX)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171009
[Lr] Data última revisão:
171009
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170912
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1367775


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[PMID]:28644059
[Au] Autor:Bozdag M; Bua S; Osman SM; AlOthman Z; Supuran CT
[Ad] Endereço:a Dipartimento di Chimica e Dipartimento Neurofarba, Sezione di Scienze Farmaceutiche e Nutraceutiche , Università degli Studi di Firenze , Florence , Italy.
[Ti] Título:Carbonic anhydrase I, II, IV and IX inhibition with a series of 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives.
[So] Source:J Enzyme Inhib Med Chem;32(1):885-892, 2017 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of new derivatives was prepared by derivatisation of the 7-amino moiety present in 7-amino-3,4-dihydroquinolin-2(1H)-one, a compound investigated earlier as CAI. The derivatisation was achieved by: i) reaction with arylsulfonyl isocyanates/aryl isocyanates; (ii) reaction with fluorescein isothiocyanate; (iii) condensation with substituted benzoic acids in the presence of carbodiimides; (iv) reaction with 2,4,6-trimethyl-pyrylium tetrafluoroborate; (v) reaction with methylsulfonyl chloride and (vi) reaction with maleic anhydride. The new compounds were assayed as inhibitors of four carbonic anhydrases (CA, EC 4.2.1.1) human (h) isoforms of pharmacologic relevance, the cytosolic hCA I and II, the membrane-anchored hCA IV and the transmembrane, tumour-associated hCA IX. hCA IX was the most inhibited isoform (K s ranging between 243.6 and 2785.6 nm) whereas hCA IV was not inhibited by these compounds. Most derivatives were weak hCA I and II inhibitors, with few of them showing K s < 10 µm. Considering that the inhibition mechanism with these lactams is not yet elucidated, exploring a range of such derivatives with various substitution patterns may be useful to identify leads showing isoform selectivity or the desired pharmacologic action.
[Mh] Termos MeSH primário: Anidrase Carbônica II/antagonistas & inibidores
Anidrase Carbônica IV/antagonistas & inibidores
Anidrase Carbônica IX/antagonistas & inibidores
Anidrase Carbônica I/antagonistas & inibidores
Inibidores da Anidrase Carbônica/farmacologia
Quinolonas/farmacologia
[Mh] Termos MeSH secundário: Anidrase Carbônica I/metabolismo
Anidrase Carbônica II/metabolismo
Anidrase Carbônica IV/metabolismo
Anidrase Carbônica IX/metabolismo
Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/química
Relação Dose-Resposta a Droga
Seres Humanos
Estrutura Molecular
Quinolonas/síntese química
Quinolonas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Quinolones); 0 (dihydroquinolin-2(1H)-one); EC 4.2.1.- (Carbonic Anhydrase I); EC 4.2.1.- (Carbonic Anhydrase II); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (Carbonic Anhydrase IX)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170624
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1337759


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[PMID]:28109946
[Au] Autor:Eldehna WM; Al-Ansary GH; Bua S; Nocentini A; Gratteri P; Altoukhy A; Ghabbour H; Ahmed HY; Supuran CT
[Ad] Endereço:Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh, Egypt. Electronic address: wagdy2000@gmail.com.
[Ti] Título:Novel indolin-2-one-based sulfonamides as carbonic anhydrase inhibitors: Synthesis, in vitro biological evaluation against carbonic anhydrases isoforms I, II, IV and VII and molecular docking studies.
[So] Source:Eur J Med Chem;127:521-530, 2017 Feb 15.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Herein we present the design, synthesis, and biological evaluation of three different series of novel sulfonamides (3a-f, 6a-f and 9a-f) incorporating substituted indolin-2-one moieties (as tails) linked to benzenesulfonamide (as zinc anchoring moieties) through aminoethyl or (4-oxothiazolidin-2-ylidene)aminoethyl linkers. The synthesized sulfonamides were evaluated in vitro for their inhibitory activity against the following human (h) carbonic anhydrase (hCA, EC 4.2.1.1) isoforms, hCA I, II, IV and VII. All these isoforms were inhibited by the sulfonamides reported here in variable degrees. hCA I was inhibited with K s in the range of 42-8550.9 nM, hCA II in the range of 5.9-761 nM; hCA IV in the range of 4.0-2069.5 nM, whereas hCA VII in the range of 13.2-694 nM. Molecular docking studies were carried out for some of the tested compounds within the hCA II active site, allowed us to rationalize the obtained inhibition results.
[Mh] Termos MeSH primário: Inibidores da Anidrase Carbônica/síntese química
Inibidores da Anidrase Carbônica/farmacologia
Anidrases Carbônicas/metabolismo
Indóis/química
Simulação de Acoplamento Molecular
Sulfonamidas/síntese química
Sulfonamidas/farmacologia
[Mh] Termos MeSH secundário: Anidrase Carbônica I/antagonistas & inibidores
Anidrase Carbônica II/antagonistas & inibidores
Anidrase Carbônica IV/antagonistas & inibidores
Inibidores da Anidrase Carbônica/química
Inibidores da Anidrase Carbônica/metabolismo
Anidrases Carbônicas/química
Domínio Catalítico
Técnicas de Química Sintética
Desenho de Drogas
Seres Humanos
Isoenzimas/antagonistas & inibidores
Isoenzimas/química
Isoenzimas/metabolismo
Relação Estrutura-Atividade
Sulfonamidas/química
Sulfonamidas/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Indoles); 0 (Isoenzymes); 0 (Sulfonamides); 0 (indolin-2-one); EC 4.2.1.- (Carbonic Anhydrase I); EC 4.2.1.- (Carbonic Anhydrase II); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (Carbonic Anhydrases); EC 4.2.1.1 (carbonic anhydrase VI)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170221
[Lr] Data última revisão:
170221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170123
[St] Status:MEDLINE


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[PMID]:27860283
[Au] Autor:Noor SI; Pouyssegur J; Deitmer JW; Becker HM
[Ad] Endereço:Division of General Zoology, Department of Biology, University of Kaiserslautern, Germany.
[Ti] Título:Integration of a 'proton antenna' facilitates transport activity of the monocarboxylate transporter MCT4.
[So] Source:FEBS J;284(1):149-162, 2017 Jan.
[Is] ISSN:1742-4658
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Monocarboxylate transporters (MCTs) mediate the proton-coupled transport of high-energy metabolites like lactate and pyruvate and are expressed in nearly every mammalian tissue. We have shown previously that transport activity of MCT4 is enhanced by carbonic anhydrase II (CAII), which has been suggested to function as a 'proton antenna' for the transporter. In the present study, we tested whether creation of an endogenous proton antenna by introduction of a cluster of histidine residues into the C-terminal tail of MCT4 (MCT4-6xHis) could facilitate MCT4 transport activity when heterologously expressed in Xenopus oocytes. Our results show that integration of six histidines into the C-terminal tail does indeed increase transport activity of MCT4 to the same extent as did coexpression of MCT4-WT with CAII. Transport activity of MCT4-6xHis could be further enhanced by coexpression with extracellular CAIV, but not with intracellular CAII. Injection of an antibody against the histidine cluster into MCT4-expressing oocytes decreased transport activity of MCT4-6xHis, while leaving activity of MCT4-WT unaltered. Taken together, these findings suggest that transport activity of the proton-coupled monocarboxylate transporter MCT4 can be facilitated by integration of an endogenous proton antenna into the transporter's C-terminal tail.
[Mh] Termos MeSH primário: Anidrase Carbônica II/metabolismo
Anidrase Carbônica IV/metabolismo
Histidina/metabolismo
Transportadores de Ácidos Monocarboxílicos/metabolismo
Proteínas Musculares/metabolismo
Oligopeptídeos/metabolismo
Prótons
Proteínas Recombinantes de Fusão/metabolismo
[Mh] Termos MeSH secundário: Animais
Anticorpos Neutralizantes/farmacologia
Transporte Biológico/efeitos dos fármacos
Anidrase Carbônica II/genética
Anidrase Carbônica IV/genética
Expressão Gênica
Histidina/antagonistas & inibidores
Histidina/genética
Ácido Láctico/metabolismo
Microinjeções
Transportadores de Ácidos Monocarboxílicos/genética
Proteínas Musculares/genética
Oligopeptídeos/antagonistas & inibidores
Oligopeptídeos/genética
Oócitos/citologia
Oócitos/efeitos dos fármacos
Oócitos/metabolismo
Engenharia de Proteínas
Ácido Pirúvico/metabolismo
Ratos
Proteínas Recombinantes de Fusão/genética
Xenopus laevis
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antibodies, Neutralizing); 0 (His-His-His-His-His-His); 0 (MCT4 protein, rat); 0 (Monocarboxylic Acid Transporters); 0 (Muscle Proteins); 0 (Oligopeptides); 0 (Protons); 0 (Recombinant Fusion Proteins); 33X04XA5AT (Lactic Acid); 4QD397987E (Histidine); 8558G7RUTR (Pyruvic Acid); EC 4.2.1.- (Carbonic Anhydrase II); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (CA4 protein, human)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170622
[Lr] Data última revisão:
170622
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161119
[St] Status:MEDLINE
[do] DOI:10.1111/febs.13964


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[PMID]:26071132
[Au] Autor:Zhang J; Tsoi H; Li X; Wang H; Gao J; Wang K; Go MY; Ng SC; Chan FK; Sung JJ; Yu J
[Ad] Endereço:Institute of Digestive Disease and Department of Medicine and Therapeutics, State Key Laboratory of Digestive Disease, Li Ka Shing Institute of Health Sciences, CUHK Shenzhen Research Institute, The Chinese University of Hong Kong, Hong Kong, Hong Kong.
[Ti] Título:Carbonic anhydrase IV inhibits colon cancer development by inhibiting the Wnt signalling pathway through targeting the WTAP-WT1-TBL1 axis.
[So] Source:Gut;65(9):1482-93, 2016 Sep.
[Is] ISSN:1468-3288
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: We found that carbonic anhydrase IV (CA4), a member of the carbonic anhydrases, is silenced in colorectal cancer (CRC). We analysed its epigenetic inactivation, biological effects and prognostic significance in CRC. DESIGN: The biological functions of CA4 were determined by in vitro and in vivo tumorigenicity assays. The CA4 co-operator was identified by immunoprecipitation and mass spectrometry. CA4 downstream effectors and signalling pathways were elucidated by promoter luciferase assay, electrophoretic mobility shift assay and chromatin immunoprecipitation. The clinical impact of CA4 was assessed in 115 patients with CRC. RESULTS: CA4 was silenced in all nine CRC cell lines and 92.6% of CRC tumours. The promoter hypermethylation contributed to the inactivation of CA4, and it was detected in 75.7% of the patients with CRC. After a median follow-up of 49.3 months, multivariate analysis showed that the patients with CA4 hypermethylation had a recurrence of Stage II/III CRC. The re-expression of CA4 inhibited cell proliferation, induced apoptosis and cell cycle arrest in the G1 phase. CA4 inhibited the activity of the Wnt signalling pathway and mediated the degradation of ß-catenin. CA4 interacted with Wilms' tumour 1-associating protein (WTAP) and induced WTAP protein degradation through polyubiquitination. Moreover, CA4 promoted the transcriptional activity of Wilms' tumour 1 (WT1), an antagonist of the Wnt pathway, which resulted in the induction of transducin ß-like protein 1 (TBL1) and the degradation of ß-catenin. CONCLUSIONS: CA4 is a novel tumour suppressor in CRC through the inhibition of the Wnt signalling pathway by targeting the WTAP-WT1-TBL1 axis. CA4 methylation may serve as an independent biomarker for the recurrence of CRC.
[Mh] Termos MeSH primário: Anidrase Carbônica IV/genética
Neoplasias Colorretais
Recidiva Local de Neoplasia/genética
Via de Sinalização Wnt/genética
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Neoplasias Colorretais/diagnóstico
Neoplasias Colorretais/genética
Neoplasias Colorretais/patologia
Regulação Neoplásica da Expressão Gênica
Genes Supressores de Tumor/fisiologia
Seres Humanos
Estadiamento de Neoplasias
Proteínas Nucleares/genética
Prognóstico
Transducina/genética
Proteínas WT1/genética
beta Catenina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Nuclear Proteins); 0 (TBL1X protein, human); 0 (WT1 Proteins); 0 (WT1 protein, human); 0 (WTAP protein, human); 0 (beta Catenin); EC 3.6.5.1 (Transducin); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (CA4 protein, human)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170630
[Lr] Data última revisão:
170630
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:150614
[St] Status:MEDLINE
[do] DOI:10.1136/gutjnl-2014-308614


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[PMID]:26487715
[Au] Autor:Wandernoth PM; Mannowetz N; Szczyrba J; Grannemann L; Wolf A; Becker HM; Sly WS; Wennemuth G
[Ad] Endereço:From the Institute of Anatomy, University Hospital, University Duisburg-Essen, Hufelandstraße 55, 45122 Essen, Germany.
[Ti] Título:Normal Fertility Requires the Expression of Carbonic Anhydrases II and IV in Sperm.
[So] Source:J Biol Chem;290(49):29202-16, 2015 Dec 04.
[Is] ISSN:1083-351X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:HCO3 (-) is a key factor in the regulation of sperm motility. High concentrations of HCO3 (-) in the female genital tract induce an increase in sperm beat frequency, which speeds progress of the sperm through the female reproductive tract. Carbonic anhydrases (CA), which catalyze the reversible hydration of CO2 to HCO3 (-), represent potential candidates in the regulation of the HCO3 (-) homeostasis in sperm and the composition of the male and female genital tract fluids. We show that two CA isoforms, CAII and CAIV, are distributed along the epididymal epithelium and appear with the onset of puberty. Expression analyses reveal an up-regulation of CAII and CAIV in the different epididymal sections of the knockout lines. In sperm, we find that CAII is located in the principal piece, whereas CAIV is present in the plasma membrane of the entire sperm tail. CAII and CAIV single knockout animals display an imbalanced HCO3 (-) homeostasis, resulting in substantially reduced sperm motility, swimming speed, and HCO3 (-)-enhanced beat frequency. The CA activity remaining in the sperm of CAII- and CAIV-null mutants is 35% and 68% of that found in WT mice. Sperm of the double knockout mutant mice show responses to stimulus by HCO3 (-) or CO2 that were delayed in onset and reduced in magnitude. In comparison with sperm from CAII and CAIV double knockout animals, pharmacological loss of CAIV in sperm from CAII knockout animals, show an even lower response to HCO3 (-). These results suggest that CAII and CAIV are required for optimal fertilization.
[Mh] Termos MeSH primário: Anidrase Carbônica II/metabolismo
Anidrase Carbônica IV/metabolismo
Fertilidade
Espermatozoides/enzimologia
[Mh] Termos MeSH secundário: Animais
Catálise
Membrana Celular/enzimologia
Feminino
Fertilização
Perfilação da Expressão Gênica
Regulação da Expressão Gênica
Homeostase
Concentração de Íons de Hidrogênio
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Camundongos Knockout
Camundongos Transgênicos
Fenótipo
Motilidade Espermática
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
EC 4.2.1.- (Carbonic Anhydrase II); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (Car4 protein, mouse)
[Em] Mês de entrada:1604
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151022
[St] Status:MEDLINE
[do] DOI:10.1074/jbc.M115.698597


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[PMID]:26319697
[Au] Autor:Vujovic M; Dudazy-Gralla S; Hård J; Solsjö P; Warner A; Vennström B; Mittag J
[Ad] Endereço:Karolinska Institutet, Department of Cell and Molecular Biology, 17177 Stockholm, Sweden.
[Ti] Título:Thyroid hormone drives the expression of mouse carbonic anhydrase Car4 in kidney, lung and brain.
[So] Source:Mol Cell Endocrinol;416:19-26, 2015 Nov 15.
[Is] ISSN:1872-8057
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Thyroid hormone is a well-known regulator of brain, lung and kidney development and function. However, the molecular mechanisms by which the hormone exerts its function have remained largely enigmatic, and only a limited set of target genes have been identified in these tissues. Using a mouse model with a mutation in thyroid hormone receptor α1 (TRα1), we here demonstrate that the expression of carbonic anhydrase 4 in lung and brain of the adult animal depends on intact TRα1 signaling. In the kidney, carbonic anhydrase 4 mRNA and protein are not affected by the mutant TRα1, but are acutely repressed by thyroid hormone. However, neither lung function--as measured by respiration rate and oxygen saturation--nor urine pH levels were affected by altered carbonic anhydrase 4 levels, suggesting that other carbonic anhydrases are likely to compensate. Taken together, our findings identify a previously unknown marker of TRα1 action in brain and lung, and provide a novel negatively regulated target gene to assess renal thyroid hormone status.
[Mh] Termos MeSH primário: Encéfalo/metabolismo
Anidrase Carbônica IV/metabolismo
Rim/metabolismo
Pulmão/metabolismo
Receptores alfa dos Hormônios Tireóideos/metabolismo
Tri-Iodotironina/metabolismo
[Mh] Termos MeSH secundário: Animais
Heterozigoto
Concentração de Íons de Hidrogênio
Camundongos
Camundongos Endogâmicos C57BL
Modelos Animais
Mutação
Taxa Respiratória
Receptores alfa dos Hormônios Tireóideos/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Thyroid Hormone Receptors alpha); 06LU7C9H1V (Triiodothyronine); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (Car4 protein, mouse)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:151014
[Lr] Data última revisão:
151014
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150831
[St] Status:MEDLINE


  9 / 117 MEDLINE  
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[PMID]:25924644
[Au] Autor:Demir N; Nadaroglu H; Gungor AA; Demir Y
[Ti] Título:The effects of some tumor markers on human erythrocyte (HCA-I and HCA-II), bovine erythrocyte (BCA) and bovine lung (CA-IV) carbonic anhydrase enzyme activities in vitro.
[So] Source:Bratisl Lek Listy;116(5):330-3, 2015.
[Is] ISSN:0006-9248
[Cp] País de publicação:Slovakia
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: The influence of prostatic acid phosphatase (PAP) and human chorionic gonadotropin (HCG), tumor markers have been investigated on human erythrocyte carbonic anhydrase (HCA-I and HCA-II) and bovine erythrocyte (BCA) and bovine lung carbonic anhydrase (CA-IV) in vitro. BACKGROUND: Tumor markers are substances that can often be detected in higher-than-normal amounts in the blood, urine, or body tissues of some patients with certain types of cancer. Tumor markers are produced either by the tumor itself or by the body in response to the presence of cancer or certain benign (noncancerous) conditions. In addition to their role in cancer diagnosis, some tumor marker levels are measured before treatment to help doctors plan appropriate therapy. RESULTS AND CONCLUSION: All of the tumor markers were determined to have inhibition effect, on human CA-I, CA-II, bovine erythrocyte CA (BCA) and bovine lung CA-IV isoenzymes. The effect of each tumor marker on CA was investigated by Wilbur-Andersen method modified by Rickly et al Inhibition effects of two different tumor markers on human CA-I, CA-II, bovine erythrocyte CA (BCA) and bovine lung CA-IV isoenzymes were determined by using the CO2-Hydratase method by plotting activity % vs (tumor markers). I50 values of tumor markers exhibiting inhibition effects were found by means of these graphs (Tab.1, Fig. 2, Ref. 20).
[Mh] Termos MeSH primário: Fosfatase Ácida/farmacologia
Biomarcadores Tumorais/farmacologia
Anidrase Carbônica II/efeitos dos fármacos
Anidrase Carbônica IV/efeitos dos fármacos
Anidrase Carbônica I/efeitos dos fármacos
Inibidores da Anidrase Carbônica/farmacologia
Gonadotropina Coriônica/farmacologia
[Mh] Termos MeSH secundário: Animais
Anidrase Carbônica I/antagonistas & inibidores
Anidrase Carbônica II/antagonistas & inibidores
Anidrase Carbônica IV/antagonistas & inibidores
Anidrases Carbônicas/efeitos dos fármacos
Bovinos
Ensaios Enzimáticos
Eritrócitos/enzimologia
Seres Humanos
Técnicas In Vitro
Pulmão/enzimologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers, Tumor); 0 (Carbonic Anhydrase Inhibitors); 0 (Chorionic Gonadotropin); EC 3.1.3.2 (Acid Phosphatase); EC 3.1.3.2 (prostatic acid phosphatase); EC 4.2.1.- (Carbonic Anhydrase I); EC 4.2.1.- (Carbonic Anhydrase II); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (Carbonic Anhydrases)
[Em] Mês de entrada:1508
[Cu] Atualização por classe:161026
[Lr] Data última revisão:
161026
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150501
[St] Status:MEDLINE


  10 / 117 MEDLINE  
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[PMID]:25358084
[Au] Autor:Dudutiene V; Matuliene J; Smirnov A; Timm DD; Zubriene A; Baranauskiene L; Morkunaite V; Smirnoviene J; Michailoviene V; Juozapaitiene V; Mickeviciute A; Kazokaite J; Baksyte S; Kasiliauskaite A; Jachno J; Revuckiene J; Kisonaite M; Pilipuityte V; Ivanauskaite E; Milinaviciute G; Smirnovas V; Petrikaite V; Kairys V; Petrauskas V; Norvaisas P; Linge D; Gibieza P; Capkauskaite E; Zaksauskas A; Kazlauskas E; Manakova E; Grazulis S; Ladbury JE; Matulis D
[Ad] Endereço:Department of Biothermodynamics and Drug Design, Institute of Biotechnology, ‡Department of Bioinformatics, Institute of Biotechnology, §Department of Protein-DNA Interactions, Institute of Biotechnology, Vilnius University , V. A. GraiciuÌ…no 8, Vilnius LT-02241, Lithuania.
[Ti] Título:Discovery and characterization of novel selective inhibitors of carbonic anhydrase IX.
[So] Source:J Med Chem;57(22):9435-46, 2014 Nov 26.
[Is] ISSN:1520-4804
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Human carbonic anhydrase IX (CA IX) is highly expressed in tumor tissues, and its selective inhibition provides a potential target for the treatment of numerous cancers. Development of potent, highly selective inhibitors against this target remains an unmet need in anticancer therapeutics. A series of fluorinated benzenesulfonamides with substituents on the benzene ring was designed and synthesized. Several of these exhibited a highly potent and selective inhibition profile against CA IX. Three fluorine atoms significantly increased the affinity by withdrawing electrons and lowering the pKa of the benzenesulfonamide group. The bulky ortho substituents, such as cyclooctyl or even cyclododecyl groups, fit into the hydrophobic pocket in the active site of CA IX but not CA II, as shown by the compound's co-crystal structure with chimeric CA IX. The strongest inhibitor of recombinant human CA IX's catalytic domain in human cells achieved an affinity of 50 pM. However, the high affinity diminished the selectivity. The most selective compound for CA IX exhibited 10 nM affinity. The compound that showed the best balance between affinity and selectivity bound with 1 nM affinity. The inhibitors described in this work provide the basis for novel anticancer therapeutics targeting CA IX.
[Mh] Termos MeSH primário: Inibidores da Anidrase Carbônica/química
Anidrases Carbônicas/química
Desenho de Drogas
[Mh] Termos MeSH secundário: Benzeno/química
Calorimetria
Dióxido de Carbono/química
Anidrase Carbônica IV/química
Catálise
Domínio Catalítico
Cristalização
Cristalografia por Raios X
Seres Humanos
Concentração de Íons de Hidrogênio
Cinética
Neoplasias/tratamento farmacológico
Ligação Proteica
Conformação Proteica
Proteínas Recombinantes/química
Sulfonamidas/química
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Carbonic Anhydrase Inhibitors); 0 (Recombinant Proteins); 0 (Sulfonamides); 142M471B3J (Carbon Dioxide); EC 4.2.1.- (Carbonic Anhydrase IV); EC 4.2.1.1 (Carbonic Anhydrases); J64922108F (Benzene)
[Em] Mês de entrada:1501
[Cu] Atualização por classe:141126
[Lr] Data última revisão:
141126
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141031
[St] Status:MEDLINE
[do] DOI:10.1021/jm501003k



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