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Titolo:
DISCOVERY OF A NOVEL, POTENT, AND SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR - STUDY OF LCK-DEPENDENT AND FYNT-DEPENDENT T-CELL ACTIVATION
Autore:
HANKE JH; GARDNER JP; DOW RL; CHANGELIAN PS; BRISSETTE WH; WERINGER EJ; POLLOK K; CONNELLY PA;
Indirizzi:
PFIZER INC,PFIZER CENT RES,EASTERN POINT RD GROTON CT 06340
Titolo Testata:
The Journal of biological chemistry
fascicolo: 2, volume: 271, anno: 1996,
pagine: 695 - 701
SICI:
0021-9258(1996)271:2<695:DOANPA>2.0.ZU;2-L
Fonte:
ISI
Lingua:
ENG
Soggetto:
RETROVIRUS PROMOTER INSERTION; AMINO-TERMINAL DOMAIN; SIGNAL TRANSDUCTION; PROTEIN-KINASE; ANTIGEN RECEPTOR; CYTOPLASMIC DOMAINS; MICE LACKING; P56LCK; CD4; EXPRESSION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
50
Recensione:
Indirizzi per estratti:
Citazione:
J.H. Hanke et al., "DISCOVERY OF A NOVEL, POTENT, AND SRC FAMILY-SELECTIVE TYROSINE KINASE INHIBITOR - STUDY OF LCK-DEPENDENT AND FYNT-DEPENDENT T-CELL ACTIVATION", The Journal of biological chemistry, 271(2), 1996, pp. 695-701

Abstract

Here, we have studied the activity of a novel protein-tyrosine kinaseinhibitor that is selective for the Src family of tyrosine kinases, We have focused our study on the effects of this compound on T cell receptor-induced T cell activation, a process dependent on the activity of the Src kinases Lck and FynT. This compound is a nanomolar inhibitorof Lck and FynT, inhibits anti-CDS-induced protein-tyrosine kinase activity in T cells, demonstrates selectivity for Lck and FynT over ZAP-70, and preferentially inhibits T cell receptor-dependent anti-CD3-induced T cell proliferation over non-T cell receptor-dependent phorbol 12-myristate 13-acetate/interleukin-2 (IL-S) induced T cell proliferation, Interestingly, this compound selectively inhibits the induction ofthe IL-2 gene, but not the granulocyte macrophage colony-stimulating factor or IL-2 receptor genes, This compound offers a useful new tool for examining the role of the Lck and FynT tyrosine kinases versus ZAP-70 in T cell. activation as well as the role of other Src family kinases in receptor function.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 31/03/20 alle ore 10:35:30