Informace o publikaci

Proteasome inhibitors - molecular basis and current perspectives in multiple myeloma

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KUBICZKOVÁ Lenka POUR Luděk SEDLAŘÍKOVÁ Lenka HÁJEK Roman ŠEVČÍKOVÁ Sabina

Rok publikování 2014
Druh Článek v odborném periodiku
Časopis / Zdroj Journal of Cellular and Molecular Medicine
Fakulta / Pracoviště MU

Lékařská fakulta

Citace
Doi http://dx.doi.org/10.1111/jcmm.12279
Obor Onkologie a hematologie
Klíčová slova Bortezomib; Multiple myeloma; New-generation proteasome inhibitors
Popis Inhibition of proteasome, a proteolytic complex responsible for the degradation of ubiquitinated proteins, has emerged as a powerful strategy for treatment of multiple myeloma (MM), a plasma cell malignancy. First-in-class agent, bortezomib, has demonstrated great positive therapeutic efficacy in MM, both in pre-clinical and in clinical studies. However, despite its high efficiency, a large proportion of patients do not achieve sufficient clinical response. Therefore, the development of a second-generation of proteasome inhibitors (PIs) with improved pharmacological properties was needed. Recently, several of these new agents have been introduced into clinics including carfilzomib, marizomib and ixazomib. Further, new orally administered second-generation PI oprozomib is being investigated. This review provides an overview of main mechanisms of action of PIs in MM, focusing on the ongoing development and progress of novel anti-proteasome therapeutics.
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