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Titolo:
Novel anthracycline prodrugs
Autore:
Damen, EWP; de Groot, FMH; Scheeren, HW;
Indirizzi:
Catholic Univ Nijmegen, Dept Organ Chem, NSR Ctr Mol Struct Design & Synthesis, NL-6525 ED Nijmegen, Netherlands Catholic Univ Nijmegen Nijmegen Netherlands NL-6525 ED egen, Netherlands
Titolo Testata:
EXPERT OPINION ON THERAPEUTIC PATENTS
fascicolo: 4, volume: 11, anno: 2001,
pagine: 651 - 666
SICI:
1354-3776(200104)11:4<651:NAP>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROSTATE-SPECIFIC ANTIGEN; SENSITIVE DIPEPTIDE PRODRUGS; PLASMINOGEN-ACTIVATOR SYSTEM; TARGETED CYTOTOXIC ANALOG; BIOLOGICAL EVALUATION; CATHEPSIN-B; NUDE-MICE; SELECTIVE ACTIVATION; CANCER-CHEMOTHERAPY; DOXORUBICIN PRODRUG;
Keywords:
beta-glucuronidase; beta-lactamase; ADEPT; AMF; anthracycline; bombesin; cathepsin B; daunorubicin; doxorubicin; enzyme; GDEPT; integrin; LH-RH; NGR; plasmin; prodrug; PSA; receptor; RGD; somatostatin; spacer;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
45
Recensione:
Indirizzi per estratti:
Indirizzo: Scheeren, HW Catholic Univ Nijmegen, Dept Organ Chem, NSR Ctr Mol Struct Design & Synthesis, Toernooiveld, NL-6525 ED Nijmegen, Netherlands Catholic Univ Nijmegen Toernooiveld Nijmegen Netherlands NL-6525 ED
Citazione:
E.W.P. Damen et al., "Novel anthracycline prodrugs", EXPERT OP T, 11(4), 2001, pp. 651-666

Abstract

This paper highlights recent patents in the field of anthracycline prodrugs, which are employed in tumour-selective chemotherapy. The prodrugs can bea part of a two-step directed enzyme prodrug therapy (DEPT), which involves the localisation of the prodrug trigger at the tumour site, followed hy the administration of the prodrug and subsequent tumour-selective anthracycline release. In most cases this trigger is an enzyme. which is indirectly localised by an antibody (ADEPT) or a gene encoding for an enzyme (GDEPT). Furthermore, anthracyclines can be targeted to the tumour site via prodrug monotherapy. Anthracycline prodrugs exploiting differences in physiological conditions, such as a lower pH and a lower oxygen tension in tumour tissue compared to healthy tissue, tumour-specific enzymes, such as plasmin, cathepsin B and beta -glucuronidase are discussed. Finally, prodrugs are reviewed that home to tumour-selective receptors. Promising advances in this fieldconcern receptors that are required for angiogenesis.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/03/20 alle ore 12:00:30