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 | Acesso ao texto completo restrito à biblioteca da Embrapa Agricultura Digital. Para informações adicionais entre em contato com cnptia.biblioteca@embrapa.br. |
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Registro Completo |
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Biblioteca(s): |
Embrapa Agricultura Digital. |
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Data corrente: |
02/02/2011 |
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Data da última atualização: |
14/01/2020 |
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Tipo da produção científica: |
Resumo em Anais de Congresso |
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Autoria: |
ANJOS, E. F.; FERREIRA, P. A.; FÁTIMA, A. de; REIS, F. S.; MORAES, F. R. de; NESHICH, G.; MILANI, R.; AOYAMA, H.; FERREIRA, C. V. |
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Afiliação: |
IB/UNICAMP; IB/UNICAMP; GEQOB/UFMG; GEQOB/UFMG; IB/UNICAMP; GORAN NESHICH, CNPTIA; IB/UNICAMP; IB/UNICAMP; IB/UNICAMP. |
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Título: |
Calix[6]arene, a novel compound acting as a strong inhibitor of the low molecular weight protein tyrosine phosphatase. |
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Ano de publicação: |
2010 |
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Fonte/Imprenta: |
In: REUNIÃO ANUAL DA SOCIEDADE BRASILEIRA DE BIOQUÍMICA E BIOLOGIA MOLECULAR - SBBq, 39.; LATIN AMERICAN SYMPOSIUM ON THE MOLECULAR MECHANISMS OF SKELETAL MINERALIZATION, 1., 2010, Foz do Iguaçu, PR. Resumos... São Paulo: SBBq, 2010. |
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Páginas: |
Não paginado. |
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Idioma: |
Inglês |
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Conteúdo: |
Calix[6]arene is a macrocyclic compound of phenolic units linked by methylene group at the 2,6-positions. Besides being used as platform for the development of new drugs and as a carrier of drugs, recently some important pharmacological properties of calixarenes have been reported. The goal of this work was to examine the effect of calix[6]arene on the low molecular weight protein tyrosine phosphatase (LMWPTP) activity. The enzyme activity was determined using p-nitrophenylphosphate as substrate. A pronounced enzyme inhibition highlighted, with an IC50 value of 1.5 µM. The efficiency of inhibition remained the same even after preincubation procedure. Accordingly, by using bioinformatics approach, it was predicted that the interaction between calix[6]arene and LMWPTP occurred nearby the catalytic site. To prove that the inhibition of the LMWPTP could also occur on cells, human leukemia cells were treated with 5 µM calix[6]arene. The expression of the enzyme was not affected, but its activity was decreased. Our findings are of particular interest as LMWPTP constitutes an attractive "druggable" target for some diseases such as cancer, obesity and diabetes. |
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Palavras-Chave: |
Calixareno; Composto macrocíclico; Inibição enzimática. |
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Thesagro: |
Atividade Enzimática. |
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Thesaurus Nal: |
Aromatic compounds; Enzyme activity; Enzyme inhibition; Organic compounds. |
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Categoria do assunto: |
S Ciências Biológicas |
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Marc: |
LEADER 02299nam a2200313 a 4500
001 1875445
005 2020-01-14
008 2010 bl uuuu u00u1 u #d
100 1 $aANJOS, E. F.
245 $aCalix[6]arene, a novel compound acting as a strong inhibitor of the low molecular weight protein tyrosine phosphatase.$h[electronic resource]
260 $aIn: REUNIÃO ANUAL DA SOCIEDADE BRASILEIRA DE BIOQUÍMICA E BIOLOGIA MOLECULAR - SBBq, 39.; LATIN AMERICAN SYMPOSIUM ON THE MOLECULAR MECHANISMS OF SKELETAL MINERALIZATION, 1., 2010, Foz do Iguaçu, PR. Resumos... São Paulo: SBBq$c2010
300 $aNão paginado.
520 $aCalix[6]arene is a macrocyclic compound of phenolic units linked by methylene group at the 2,6-positions. Besides being used as platform for the development of new drugs and as a carrier of drugs, recently some important pharmacological properties of calixarenes have been reported. The goal of this work was to examine the effect of calix[6]arene on the low molecular weight protein tyrosine phosphatase (LMWPTP) activity. The enzyme activity was determined using p-nitrophenylphosphate as substrate. A pronounced enzyme inhibition highlighted, with an IC50 value of 1.5 µM. The efficiency of inhibition remained the same even after preincubation procedure. Accordingly, by using bioinformatics approach, it was predicted that the interaction between calix[6]arene and LMWPTP occurred nearby the catalytic site. To prove that the inhibition of the LMWPTP could also occur on cells, human leukemia cells were treated with 5 µM calix[6]arene. The expression of the enzyme was not affected, but its activity was decreased. Our findings are of particular interest as LMWPTP constitutes an attractive "druggable" target for some diseases such as cancer, obesity and diabetes.
650 $aAromatic compounds
650 $aEnzyme activity
650 $aEnzyme inhibition
650 $aOrganic compounds
650 $aAtividade Enzimática
653 $aCalixareno
653 $aComposto macrocíclico
653 $aInibição enzimática
700 1 $aFERREIRA, P. A.
700 1 $aFÁTIMA, A. de
700 1 $aREIS, F. S.
700 1 $aMORAES, F. R. de
700 1 $aNESHICH, G.
700 1 $aMILANI, R.
700 1 $aAOYAMA, H.
700 1 $aFERREIRA, C. V.
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Embrapa Agricultura Digital (CNPTIA) |
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