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Titolo:
3-amidinophenylalanine-based inhibitors of urokinase
Autore:
Sturzebecher, J; Vieweg, H; Steinmetzer, T; Schweinitz, A; Stubbs, MT; Renatus, M; Wikstrom, P;
Indirizzi:
Univ Jena, Zentrum F Vaskulare Biol & Med, D-99089 Erfurt, Germany Univ Jena Erfurt Germany D-99089 are Biol & Med, D-99089 Erfurt, Germany Pentapharm Ltd, CH-4002 Basel, Switzerland Pentapharm Ltd Basel Switzerland CH-4002 Ltd, CH-4002 Basel, Switzerland Univ Jena, Inst Biochem & Biophys, D-07743 Jena, Germany Univ Jena Jena Germany D-07743 Biochem & Biophys, D-07743 Jena, Germany Univ Marburg, Inst Pharmazeut Chem, D-35032 Marburg, Germany Univ MarburgMarburg Germany D-35032 zeut Chem, D-35032 Marburg, Germany Burnham Inst, La Jolla, CA 92037 USA Burnham Inst La Jolla CA USA 92037Burnham Inst, La Jolla, CA 92037 USA
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
fascicolo: 21, volume: 9, anno: 1999,
pagine: 3147 - 3152
SICI:
0960-894X(19991101)9:21<3147:3IOU>2.0.ZU;2-3
Fonte:
ISI
Lingua:
ENG
Soggetto:
PLASMINOGEN-ACTIVATOR; CANCER METASTASIS; THROMBIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
16
Recensione:
Indirizzi per estratti:
Indirizzo: Sturzebecher, J Univ Jena, Zentrum F Vaskulare Biol & Med, D-99089 Erfurt,Germany Univ Jena Erfurt Germany D-99089 D-99089 Erfurt, Germany
Citazione:
J. Sturzebecher et al., "3-amidinophenylalanine-based inhibitors of urokinase", BIOORG MED, 9(21), 1999, pp. 3147-3152

Abstract

Synthesis and anti-uPA activity of a series of N alpha-triisopropyl-phenylsulfonyl-protecte 3-amidinophenylalanine amides are described. We have explored SAR around the C-terminal amide part for inhibition of uPA, plasmin and trypsin. Modification of the amide part has been found to affect potency but not selectivity. With a K-i of 0.41 mu M 2r-L is one of the most potentuPA inhibitors described so far. The X-ray crystal structure of 2r-L was solved in complex with trypsin, superimposed with uPA and the results suggest an unique binding mode of this inhibitor type. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/07/20 alle ore 11:40:21