Abstract
Proteasomes have a fundamental function since they degrade numerous different proteins, including those involved in the regulation of the cell cycle. Proteasome inhibition is a novel approach to the treatment of solid tumours. PS-341 (bortezomib) is a small, cell-permeable molecule that selectively inhibits the proteasome binding it in a reversible manner. The proteasome has been established as an important target in haematologic malignancies and has been approved for the treatment of multiple myeloma. Bortezomib induces apoptosis of malignant cells through the inhibition of NF-κB and stabilisation of proapoptotic proteins. In preclinical studies, bortezomib also promoted chemo and radiosensitisation of malignant cells in vitro and inhibited tumour growth in murine xenografts models. The single-agent and combination studies of bortezomib in solid tumours are detailed.
| Original language | English |
|---|---|
| Pages (from-to) | 1125-1133 |
| Number of pages | 9 |
| Journal | European Journal of Cancer |
| Volume | 43 |
| Issue number | 7 |
| DOIs | |
| Publication status | Published - May 2007 |
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Keywords
- Apoptosis
- Bortezomib
- Clinical studies
- Cyclin-dependent kinase
- Cyclins
- Multiple myeloma
- NF-κB
- Preclinical studies
- Proteasome
- Solid tumours
ASJC Scopus subject areas
- Cancer Research
- Hematology
- Oncology
Cite this
The proteasome : A worthwhile target for the treatment of solid tumours? / Milano, Amalia; Iaffaioli, Rosario Vincenzo; Caponigro, Francesco.
In: European Journal of Cancer, Vol. 43, No. 7, 05.2007, p. 1125-1133.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - The proteasome
T2 - A worthwhile target for the treatment of solid tumours?
AU - Milano, Amalia
AU - Iaffaioli, Rosario Vincenzo
AU - Caponigro, Francesco
PY - 2007/5
Y1 - 2007/5
N2 - Proteasomes have a fundamental function since they degrade numerous different proteins, including those involved in the regulation of the cell cycle. Proteasome inhibition is a novel approach to the treatment of solid tumours. PS-341 (bortezomib) is a small, cell-permeable molecule that selectively inhibits the proteasome binding it in a reversible manner. The proteasome has been established as an important target in haematologic malignancies and has been approved for the treatment of multiple myeloma. Bortezomib induces apoptosis of malignant cells through the inhibition of NF-κB and stabilisation of proapoptotic proteins. In preclinical studies, bortezomib also promoted chemo and radiosensitisation of malignant cells in vitro and inhibited tumour growth in murine xenografts models. The single-agent and combination studies of bortezomib in solid tumours are detailed.
AB - Proteasomes have a fundamental function since they degrade numerous different proteins, including those involved in the regulation of the cell cycle. Proteasome inhibition is a novel approach to the treatment of solid tumours. PS-341 (bortezomib) is a small, cell-permeable molecule that selectively inhibits the proteasome binding it in a reversible manner. The proteasome has been established as an important target in haematologic malignancies and has been approved for the treatment of multiple myeloma. Bortezomib induces apoptosis of malignant cells through the inhibition of NF-κB and stabilisation of proapoptotic proteins. In preclinical studies, bortezomib also promoted chemo and radiosensitisation of malignant cells in vitro and inhibited tumour growth in murine xenografts models. The single-agent and combination studies of bortezomib in solid tumours are detailed.
KW - Apoptosis
KW - Bortezomib
KW - Clinical studies
KW - Cyclin-dependent kinase
KW - Cyclins
KW - Multiple myeloma
KW - NF-κB
KW - Preclinical studies
KW - Proteasome
KW - Solid tumours
UR - http://www.scopus.com/inward/record.url?scp=34247125164&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=34247125164&partnerID=8YFLogxK
U2 - 10.1016/j.ejca.2007.01.038
DO - 10.1016/j.ejca.2007.01.038
M3 - Article
C2 - 17379504
AN - SCOPUS:34247125164
VL - 43
SP - 1125
EP - 1133
JO - European Journal of Cancer
JF - European Journal of Cancer
SN - 0959-8049
IS - 7
ER -