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Entry into a new class of potent proteasome inhibitors having high antiproliferative activity by structure-based design
Authors:Furet Pascal  Imbach Patricia  Noorani Maria  Koeppler Juergen  Laumen Kurt  Lang Marc  Guagnano Vito  Fuerst Peter  Roesel Johannes  Zimmermann Johann  García-Echeverría Carlos
Affiliation:Novartis Pharma AG, Novartis Institutes for Biomedical Research, CH-4002 Basel, Switzerland.
Abstract:
Proteasome inhibition is a therapeutic concept of current interest in anticancer research. We report here the design, synthesis, and biological characterization of prototypes of a new class of noncovalent proteasome inhibitors showing high activity in biochemical and cellular assays.
Keywords:
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