Proteasome inhibitors in cancer therapy

被引：0

作者：

Romaniuk, Wioletta ^{[1
]}

Oldziej, Agnieszka Ewa ^{[1
]}

Zinczuk, Justyna ^{[2
]}

Kloczko, Janusz ^{[1
]}

机构：

[1] Uniwersytet Med Bialymstoku, Klin Hematol, Pododdzialem Chorob Naczyn, Bialystok, Poland

[2] Uniwersytet Med Bialymstoku, Zaklad Patomorfol Ogolnej, Bialystok, Poland

来源：

POSTEPY HIGIENY I MEDYCYNY DOSWIADCZALNEJ | 2015年 / 69卷

关键词：

proteasome; carfilzomib; ixazomib; delanzomib; oprozomib; marizomib; SINGLE-AGENT CARFILZOMIB; CELLS IN-VITRO; IRREVERSIBLE INHIBITOR; PRECLINICAL MODELS; ANTITUMOR-ACTIVITY; DRUG-RESISTANCE; MULTIPLE; LENALIDOMIDE; COMBINATION; CEP-18770;

D O I：

暂无

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Proteasomes are multisubunit enzyme complexes. They contain three enzymatic active sites which are termed chymotrypsin-like, trypsin-like, and caspase-like. The elementary function of the proteasomes is degradation of damaged proteins. Proteasome inhibition leads to accumulation of damaged protein, which leads to caspase activation and cell death. This relationship is used in cancer therapy. Bortezomib is the first proteasome inhibitor approved by the US Food and Drug Administration for the treatment of relapsed/refractory multiple myeloma. Carfilzomib belongs to the second generation of drugs, which was approved by the US FDA in 2012. Currently in the study phase there are four new inhibitors: ixazomib (MLN9780/MLN2238), delanzomib (CEP-18770), oprozomib (ONX0912/PR-047) and marizomib (NPI-0052).

引用

页码：1443 / 1450

页数：8

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