Classification and synthesis of ubiquitin-proteasome inhibitor / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1313-1319, 2009.
Article
in Chinese
| WPRIM
| ID: wpr-344078
ABSTRACT
The inhibition of protein degradation through the ubiquitin-proteasome pathway is a recently developed approach to cancer treatment which extends the range of cellular target for chemotherapy. This therapeutic strategy is very interesting since the proteasomes carry out the regulated degradation of unnecessary or damaged cellular proteins, a process that is dysregulated in many cancer cells. Based on this hypothesis, the proteasome complex inhibitor Bortezomib was approved for use in multiple myeloma patients by FDA in 2003. Drug discovery programs in academy and the pharmaceutical industry have developed a range of synthetic and natural inhibitors of the 20S proteasome core particle that have entered human clinical trials as significant anti-cancer leads. The main results from the use of proteasome inhibition in cancer chemotherapy, the structure of several proteasome inhibitors and their synthesis is going to be reviewed in this paper.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Peptides, Cyclic
/
Acetylcysteine
/
Pyrazines
/
Boronic Acids
/
Cysteine Proteinase Inhibitors
/
Chemistry
/
Classification
/
Ubiquitin
/
Therapeutic Uses
/
Proteasome Endopeptidase Complex
Limits:
Humans
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2009
Type:
Article
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