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Titolo:
A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells
Autore:
Lane, ME; Yu, B; Rice, A; Lipson, KE; Liang, C; Sun, L; Tang, C; McMahon, G; Pestell, RG; Wadler, S;
Indirizzi:
Yeshiva Univ Albert Einstein Coll Med, Dept Med, Div Oncol, Bronx, NY 10461 USA Yeshiva Univ Albert Einstein Coll Med Bronx NY USA 10461 nx, NY 10461 USA Albert Einstein Canc Ctr, Bronx, NY 10461 USA Albert Einstein Canc Ctr Bronx NY USA 10461 Canc Ctr, Bronx, NY 10461 USA SUGEN, S San Francisco, CA 94080 USA SUGEN S San Francisco CA USA 94080SUGEN, S San Francisco, CA 94080 USA
Titolo Testata:
CANCER RESEARCH
fascicolo: 16, volume: 61, anno: 2001,
pagine: 6170 - 6177
SICI:
0008-5472(20010815)61:16<6170:ANCISI>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
CYCLIN-DEPENDENT KINASES; TRANSCRIPTION FACTOR E2F-1; GROWTH-FACTOR RECEPTOR; S-PHASE ENTRY; RETINOBLASTOMA PROTEIN; DNA-BINDING; COLORECTAL CARCINOMAS; G(1) ARREST; HUMAN CDK2; CANCER;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
66
Recensione:
Indirizzi per estratti:
Indirizzo: Wadler, S Montefiore Med Ctr, Dept Oncol, 111 E 210th St,HOF 100, Bronx, NY 10467 USA Montefiore Med Ctr 111 E 210th St,HOF 100 Bronx NY USA 10467 USA
Citazione:
M.E. Lane et al., "A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells", CANCER RES, 61(16), 2001, pp. 6170-6177

Abstract

Recent studies have indicated that the development of cyclin-dependent kinase (cdk)2 inhibitors that deregulate E2F are a plausible pharmacological strategy for novel antineoplastic agents. We show here that 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516), a novel 3-substituted indolinone compound, binds to and selectively inhibits theactivity of cdk2. This inhibition results in a time-dependent decrease (4-64%) in the phosphorylation of the retinoblastoma protein pRb, an increase in caspase-3 activation (5-84%), and alterations in cell cycle resulting ineither a G(0)-G(1) or a G-NI block. We also report here cell line differences in the cdk-dependent phosphorylation of pRb. These findings demonstratethat SU9516 is a selective cdk2 inhibitor and support the theory that compounds Thai inhibit cdk2 are viable resources in the development of new antineoplastic agents.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/04/20 alle ore 02:15:52