Development of peptidomimetic boronates as proteasome inhibitors

…, C Di Giovanni, K Scarbaci, V Troiano, S Grasso…

Index: Micale, Nicola; Ettari, Roberta; Lavecchia, Antonio; Di Giovanni, Carmen; Scarbaci, Kety; Troiano, Valeria; Grasso, Silvana; Novellino, Ettore; Schirmeister, Tanja; Zappala, Maria European Journal of Medicinal Chemistry, 2013 , vol. 64, p. 23 - 34

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Citation Number: 17

Abstract

Proteasome inhibition has emerged over the past decade as an effective therapeutic approach for the treatment of hematologic malignancies. It is a multicatalytic complex, whose proteolytic activity relies in three types of subunits: chymotrypsin-like (β5), trypsin-like (β2) and caspase-like (β1). Most important for the development of effective antitumor agents is the inhibition of the β5 subunits. In this context, the dipeptide boronate bortezomib ( ...