Bortezomib as an antitumor agent.
Curr Pharm Biotechnol
; 7(6): 441-8, 2006 Dec.
Article
em En
| MEDLINE
| ID: mdl-17168660
ABSTRACT
The ubiquitin-proteasome pathway (UPP) is the major non-lysosomal proteolytic system in the cytosol and nucleus of all eukaryotic cells. Bortezomib (also known as PS-341 and Velcade) is a proteasome inhibitor, a novel class of cancer therapies. Bortezomib blocks multi-ubiquitinated protein degradation by inhibiting 26S proteasome activity, including regulating cell cycle, anti-apoptosis, and inflammation, as well as immune surveillance. In multiple myeloma (MM) cells, bortezomib directly induces cell stress response followed by activation of c-Jun NH(2) terminal kinase (JNK)/stress-activated protein kinase (SAPK), and triggers caspase-dependent apoptosis of tumor cells. Recent clinical studies demonstrated that bortezomib had remarkable anti-tumor activity in refractory and relapsed MM, providing the basis to approval by FDA. Its anti-tumor activities earlier in the course, in combination therapies, and in other malignancies is ongoing.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirazinas
/
Ácidos Borônicos
/
Transdução de Sinais
/
Ubiquitina
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Complexo de Endopeptidases do Proteassoma
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Mieloma Múltiplo
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article