Development of proteasome inhibitors for the treatment of multiple myeloma

Result code in IS VaVaI
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Result on the web
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DOI - Digital Object Identifier
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Result language
angličtina
Original language name
Development of proteasome inhibitors for the treatment of multiple myeloma
Original language description
This chapter provides a comprehensive review of the new proteasome inhibitors (PI) generation with the higher efficacy of proteasome inhibition, the enhanced antitumor activity and the decreased toxicity. Carfilzomib (Kyprolis, PR-171) is an irreversibletetrapeptide PI that belongs to the epoxyketone class and is structurally and mechanistically distinct from bortezomib. Carfilzomib has demonstrated activity against bortezomib-resistant cell lines and primary multiple myeloma (MM) cells. Marizomib (NPI-0052, salinosporamide A) is a natural lactone compound derived from the marine bacterium Salinospora tropica and belongs to a unique class of PIs, the salinosporamides. Ixazomib (MLN-2238, the biologically active form of MLN-9708), a dipeptidilic boronic acid, has improved pharmacokinetics, pharmacodynamics, and antitumor activity in preclinical studies, compared with bortezomib. Oprozomib (ONX 0912 and PR 047) and Delanzomib (CEP-18770) are orally bioavailable PIs
Czech name
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Czech description
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Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2014
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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