Data/hora: 20/06/2024 03:26:17

Biblioteca(s): | Embrapa Agricultura Digital.
Data corrente: | 02/02/2011
Data da última atualização: | 14/01/2020
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.
Afiliação: | IB/UNICAMP; IB/UNICAMP; GEQOB/UFMG; GEQOB/UFMG; IB/UNICAMP; GORAN NESHICH, CNPTIA; IB/UNICAMP; IB/UNICAMP; IB/UNICAMP.
Título: | Calix[6]arene, a novel compound acting as a strong inhibitor of the low molecular weight protein tyrosine phosphatase.
Ano de publicação: | 2010
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.
Páginas: | Não paginado.
Idioma: | Inglês
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.
Palavras-Chave: | Calixareno; Composto macrocíclico; Inibição enzimática.
Thesagro: | Atividade Enzimática.
Thesaurus Nal: | Aromatic compounds; Enzyme activity; Enzyme inhibition; Organic compounds.
Categoria do assunto: | S Ciências Biológicas
Registro original: | Embrapa Agricultura Digital (CNPTIA)
Exemplares: | CNPTIA - (15534-1) - UPC - RA - DD -  -  -  - DIS