Calix[6]arene, a novel compound acting as a strong inhibitor of the low molecular weight protein tyrosine phosphatase.

AUTOR(ES)
FONTE

REUNIÃO ANUAL DA SOCIEDADE BRASILEIRA DE BIOQUÍMICA E BIOLOGIA MOLECULAR ? SBBq

DATA DE PUBLICAÇÃO

2011

RESUMO

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.

ASSUNTO(S)

calixareno composto macrocíclico atividade enzimática inibição enzimática organic compounds aromatic compounds enzyme activity enzyme inhibition

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