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Titolo:
Extracellularly tumor-activated prodrugs for the selective chemotherapy ofcancer: Application to doxorubicin and preliminary in vitro and in vivo studies
Autore:
Trouet, A; Passioukov, A; Van Derpoorten, K; Fernandez, AM; Abarca-Quinones, J; Baurain, R; Lobl, TJ; Oliyai, C; Shochat, D; Dubois, V;
Indirizzi:
Univ Catholique Louvain, Cell Biol Lab, B-1348 Louvain, Belgium Univ Catholique Louvain Louvain Belgium B-1348 , B-1348 Louvain, Belgium Corixa, S San Francisco, CA 94080 USA Corixa S San Francisco CA USA 94080Corixa, S San Francisco, CA 94080 USA
Titolo Testata:
CANCER RESEARCH
fascicolo: 7, volume: 61, anno: 2001,
pagine: 2843 - 2846
SICI:
0008-5472(20010401)61:7<2843:ETPFTS>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
L-LEUCYL-DOXORUBICIN; PROSTATE-SPECIFIC ANTIGEN; IN-VIVO; XENOGRAFTS; PHARMACOKINETICS; ANTHRACYCLINES; DERIVATIVES; PLASMIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Clinical Medicine
Life Sciences
Citazioni:
17
Recensione:
Indirizzi per estratti:
Indirizzo: Trouet, A Univ Catholique Louvain, Cell Biol Lab, Pl Croix Sud 5, B-1348 Louvain, Belgium Univ Catholique Louvain Pl Croix Sud 5 Louvain Belgium B-1348 m
Citazione:
A. Trouet et al., "Extracellularly tumor-activated prodrugs for the selective chemotherapy ofcancer: Application to doxorubicin and preliminary in vitro and in vivo studies", CANCER RES, 61(7), 2001, pp. 2843-2846

Abstract

Oligopeptidic derivatives of anthracyclines unable to penetrate cells wereprepared and screened for their stability in human blood and their reactivation by peptidases secreted by cancer cells. N-beta -alanyl-L-leucyl-L-alanyl-L-leucyl-doxorubicin was selected as a new candidate prodrug, The NH2-terminal beta -alanine allows a very good blood stability, A two-step activation by peptidases found in conditioned media of cancer cells ultimately yields N-L-leucyl-doxorubicin. In vitro, when MCF-7/6 cancer cells are exposed to the prodrug, they accumulate about 14 times more doxorubicin than MRC-5 normal fibroblasts, whereas when exposed to doxorubicin the uptake is slightly higher in fibroblasts than in MCF-7/6 cells. This increased specificity of the prodrug over doxorubicin was confirmed in cytotoxicity assays using the same cell types. In vivo, the prodrug proved about nine times less toxic than doxorubicin in the normal mouse and also much more efficient in two different experimental chemotherapy models of human breast tumors.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/12/20 alle ore 18:24:27