Document Detail

Analysing properties of proteasome inhibitors using kinetic and X-ray crystallographic studies.
MedLine Citation:
PMID:  22350899     Owner:  NLM     Status:  MEDLINE    
The combination of X-ray crystallography and kinetic studies of proteasome:ligand complexes has proven to be an important tool in inhibitor analysis of this crucial protein degradation machinery. Here, we describe in detail the purification protocols, proteolytic activity assays, crystallisation methods, and structure determination for the yeast 20S proteasome (CP) in complex with its inhibitors. The fusion of these advanced techniques offers the opportunity to further optimise drugs which are already tested in different clinical phase studies, as well as to design new promising proteasome lead structures which might be suitable for their application in medicine, plant protection, and antibiotics.
Nerea Gallastegui; Michael Groll
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Methods in molecular biology (Clifton, N.J.)     Volume:  832     ISSN:  1940-6029     ISO Abbreviation:  Methods Mol. Biol.     Publication Date:  2012  
Date Detail:
Created Date:  2012-02-21     Completed Date:  2012-07-16     Revised Date:  2013-08-14    
Medline Journal Info:
Nlm Unique ID:  9214969     Medline TA:  Methods Mol Biol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  373-90     Citation Subset:  IM    
Department of Biochemistry, Technische Universität München, Garching, Germany.
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MeSH Terms
Antineoplastic Agents / analysis
Boronic Acids / pharmacology
Crystallography, X-Ray / methods*
Drug Design*
Enzyme Inhibitors / analysis*,  chemistry*
Lactones / pharmacology
Multiple Myeloma / drug therapy
Oligopeptides / pharmacology
Proteasome Endopeptidase Complex / genetics,  metabolism
Proteasome Inhibitors*
Pyrazines / pharmacology
Pyrroles / pharmacology
Saccharomyces cerevisiae / metabolism
Threonine / analogs & derivatives,  pharmacology
Reg. No./Substance:
0/Antineoplastic Agents; 0/Boronic Acids; 0/Enzyme Inhibitors; 0/Lactones; 0/Oligopeptides; 0/Proteasome Inhibitors; 0/Pyrazines; 0/Pyrroles; 0/bortezomib; 0/carfilzomib; 0/marizomib; 6IF28942WO/delanzomib; 72-19-5/Threonine; EC Endopeptidase Complex

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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