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Titolo:
Prodrug strategies in cancer therapy
Autore:
Denny, WA;
Indirizzi:
Univ Auckland, Fac Med & Hlth Sci, Auckland Canc Soc, Res Ctr, Auckland 1,New Zealand Univ Auckland Auckland New Zealand 1 oc, Res Ctr, Auckland 1,New Zealand
Titolo Testata:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 7-8, volume: 36, anno: 2001,
pagine: 577 - 595
SICI:
0223-5234(200107/08)36:7-8<577:PSICT>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
SELECTIVE ANTITUMOR AGENTS; BIOREDUCTIVE ALKYLATING-AGENTS; ESCHERICHIA-COLI-B; CELL LUNG-CANCER; ADVANCED MALIGNANT-MELANOMA; HYPOXIC MAMMALIAN-CELLS; ACUTE MYELOID-LEUKEMIA; NITRACRINE N-OXIDE; C P-450 REDUCTASE; PHASE-II TRIAL;
Keywords:
ADEPT; armed antibodies; GDEPT; hypoxia; peptide conjugates; tumour-activated prodrugs;
Tipo documento:
Review
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
182
Recensione:
Indirizzi per estratti:
Indirizzo: Denny, WA Univ Auckland, Fac Med & Hlth Sci, Auckland Canc Soc, Res Ctr, Private Bag92019, Auckland 1, New Zealand Univ Auckland Private Bag 92019 Auckland New Zealand 1 Zealand
Citazione:
W.A. Denny, "Prodrug strategies in cancer therapy", EUR J MED C, 36(7-8), 2001, pp. 577-595

Abstract

Systemic cytotoxic (anti-proliferative) anticancer drugs rely primarily for their therapeutic effect on cytokinetic differences between cancer and normal cells. One approach aimed, at improving the selectivity of tumour cellkilling by such compounds is the use of less toxic prodrug forms that can be selectively activated in tumour tissue (tumour-activated prodrugs; TAP). There are several mechanisms potentially exploitable for selective activation. Some utilise unique aspects of tumour physiology such as selective enzyme expression, hypoxia, and low extracellular pH. Others are based on tumour-specific delivery techniques, including activation of prodrugs by exogenous enzymes delivered to tumour cells via monoclonal antibodies (ADEPT), orgenerated in turnout cells from DNA constructs containing the corresponding gene (GDEPT). Because only a small proportion of the tumour cells may be competent to activate the prodrug, whichever activating mechanism is used, TAP need to be capable of killing activation-incompetent cells as well via a "bystander effect", in order to fully,exploit these "activator" cells. A wide variety of chemistries have been explored for the selective activationof TAP. These include reduction of quinones, N-oxides, nitroaromatics and metal complexes by endogenous enzymes or radiation, amide cleavage by endogenous peptidases, and metabolism by a variety of exogenous enzymes, including phosphatases, kinases, amidases and glycosidases. (C) 2001 Editions scientifiques et medicales Elsevier SAS.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/09/20 alle ore 16:41:06