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Titolo:
Development and in vitro efficacy of novel MMP2 and MMP9 specific doxorubicin albumin conjugates
Autore:
Kratz, F; Drevs, J; Bing, G; Stockmar, C; Scheuermann, K; Lazar, P; Unger, C;
Indirizzi:
Tumor Biol Ctr, D-79106 Freiburg, Germany Tumor Biol Ctr Freiburg Germany D-79106 l Ctr, D-79106 Freiburg, Germany
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 15, volume: 11, anno: 2001,
pagine: 2001 - 2006
SICI:
0960-894X(20010806)11:15<2001:DAIVEO>2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN-SERUM-ALBUMIN; MATRIX METALLOPROTEINASES; DRUG-CARRIER; INVIVO; DAUNOMYCIN; INHIBITORS; INVITRO; ASSAYS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
18
Recensione:
Indirizzi per estratti:
Indirizzo: Kratz, F Tumor Biol Ctr, D-79106 Freiburg, Germany Tumor Biol Ctr Freiburg Germany D-79106 79106 Freiburg, Germany
Citazione:
F. Kratz et al., "Development and in vitro efficacy of novel MMP2 and MMP9 specific doxorubicin albumin conjugates", BIOORG MED, 11(15), 2001, pp. 2001-2006

Abstract

Two doxorubicin albumin conjugates (A-DP1 and A-DP2), which differ in their substrate specificity fur the matrix metalloproteinases MMP2 and MMP9. were prepared by binding maleimide doxorubicin peptide derivatives to the cysteine-34 position of human serum albumin. The incorporated octapeptide, Gly-Pro-Gln-Arg-Ile-Ala-Giy-Gln, in A-DP2 is not cleaved by activated MMP2 andMMP9 in contrast to Gly-Pro-Leu-Gly-Ile-Ala-Gly-Gln incorporated in A-DP1 that is cleaved efficiently by activated MMP2 and MMP9 liberating a doxorubicin tetrapeptide. A-DP1 showed antiproliferative activity in a murine renal cell carcinoma line in the low micromolar range (IC50 value approximate to0.2 muM). (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 09/04/20 alle ore 06:01:37