Bis(N,N-dimethylhydroxamido)hydroxooxovanadate inhibition of protein tyrosine phosphatase activity in intact cells: comparison with vanadate.
Biochem Pharmacol
; 58(12): 1859-67, 1999 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-10591140
ABSTRACT
We have shown previously that bis(N,N-dimethylhydroxamido)hydroxooxovanadate (DMHV) is an excellent reversible inhibitor of protein tyrosine phosphatase (PTP) in vitro. DMHV does not carry a charge under physiological pH conditions and is anticipated to permeate cell membranes more easily than vanadate. In the present study, the efficacy of DMHV as a PTP inhibitor in intact cells was compared with that of vanadate by measuring phosphotyrosine levels in various cells treated with these compounds. DMHV was more effective in increasing both the phosphotyrosine levels of various proteins in 3T3L1 fibroblasts and the level of insulin-receptor phosphorylation in CHO cells overexpressing the human insulin receptor. DMHV was about 10- to 20-fold more effective than vanadate in increasing glucose transport and glycogen synthesis in 3T3L1 adipocytes. DMHV, unlike vanadate, also inhibited PTP in Jurkat cells. The implications of these observations are discussed.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Vanadatos
/
Proteínas Tirosina Fosfatases
/
Inibidores Enzimáticos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Biochem Pharmacol
Ano de publicação:
1999
Tipo de documento:
Article
País de afiliação:
Canadá