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  Epoxysuccinyl peptide-derived cathepsin B inhibitors: Modulating membrane permeability by conjugation with the C- terminal heptapeptide segment of penetratin

Schaschke, N., Deluca, D., Assfalg-Machleidt, I., Höhneke, C., Sommerhoff, C. P., & Machleidt, W. (2002). Epoxysuccinyl peptide-derived cathepsin B inhibitors: Modulating membrane permeability by conjugation with the C- terminal heptapeptide segment of penetratin. Biological Chemistry, 383(5), 849-852.

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Genre: Zeitschriftenartikel
Alternativer Titel : Biol. Chem.

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 Urheber:
Schaschke, N.1, Autor           
Deluca, D.2, Autor           
Assfalg-Machleidt, I.2, Autor           
Höhneke, C., Autor
Sommerhoff, C. P., Autor
Machleidt, W.2, Autor           
Affiliations:
1Moroder, Luis / Bioorganic Chemistry, Max Planck Institute of Biochemistry, Max Planck Society, ou_1565160              
2External Organizations, ou_persistent22              

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Schlagwörter: antennapedia; CA074; cathepsin L; MCF-7 cells
 Zusammenfassung: Besides its physiological role in lysosomal protein breakdown, extralysosomal cathepsin B has recently been implicated in apoptotic cell death. Highly specific irreversible cathepsin B inhibitors that are readily cellpermeant should be useful tools to elucidate the effects of cathepsin B in the cytosol. We have covalently functionalised the poorly cellpermeant epoxysuccinyl based cathepsin B inhibitor [RGlyGlyLeu(2S, 3S)tEpsLeuProOH; R=OMe] with the Cterminal heptapeptide segment of penetratin (R=[epsilon]AhxArg ArgNleLysTrpLysLysNH(2)). The high inhibitory potency and selectivity for cathepsin B versus cathepsin L of the parent compound was not affected by the conjugation with the penetratin heptapeptide. The conjugate was shown to efficiently penetrate into MCF-7 cells as an active inhibitor, thereby circumventing an intracellular activation step that is required by other inhibitors, such as the prodruglike epoxysuccinyl peptides E64d and CA074Me.

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Sprache(n): eng - English
 Datum: 2002-05
 Publikationsstatus: Erschienen
 Seiten: -
 Ort, Verlag, Ausgabe: -
 Inhaltsverzeichnis: -
 Art der Begutachtung: Expertenbegutachtung
 Identifikatoren: eDoc: 31323
ISI: 000176382200016
 Art des Abschluß: -

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Titel: Biological Chemistry
  Alternativer Titel : Biol. Chem.
Genre der Quelle: Zeitschrift
 Urheber:
Affiliations:
Ort, Verlag, Ausgabe: -
Seiten: - Band / Heft: 383 (5) Artikelnummer: - Start- / Endseite: 849 - 852 Identifikator: ISSN: 1431-6730