Potent and selective inhibitors of the proteasome: Dipeptidyl boronic acids

Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases. Pot...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-02, Vol.8 (4), p.333-338
Hauptverfasser:	Adams, Julian, Behnke, Mark, Chen, Shaowu, Cruickshank, Amy A., Dick, Lawrence R., Grenier, Louis, Klunder, Janice M., Ma, Yu-Ting, Plamondon, Louis, Stein, Ross L.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Biological and medical sciences Boronic Acids - chemistry Boronic Acids - pharmacology Cysteine Endopeptidases - drug effects General aspects Medical sciences Molecular Structure Multienzyme Complexes - drug effects Pharmacology. Drug treatments Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Proteasome Endopeptidase Complex
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Beschreibung
Zusammenfassung:	Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases. Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for treatment of cancer and inflammatory diseases.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00029-8