2f16
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(New page: 200px<br /><applet load="2f16" size="450" color="white" frame="true" align="right" spinBox="true" caption="2f16, resolution 2.8Å" /> '''Crystal structure of ...)
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Revision as of 08:10, 21 November 2007
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Crystal structure of the yeast 20S proteasome in complex with bortezomib
Overview
The dipeptide boronic acid bortezomib, also termed VELCADE, is a, proteasome inhibitor now in use for the treatment of multiple myeloma, and, its use for the treatment of other malignancies is being explored. We, determined the crystal structure of the yeast 20S proteasome in complex, with bortezomib to establish the specificity and binding mode of, bortezomib to the proteasome's different catalytically active sites. This, structure should enable the rational design of new boronic acid, derivatives with improved affinities and specificities for individual, active subunits.
About this Structure
2F16 is a Protein complex structure of sequences from Saccharomyces cerevisiae with BO2 as ligand. Active as Proteasome endopeptidase complex, with EC number 3.4.25.1 Full crystallographic information is available from OCA.
Reference
Crystal structure of the boronic acid-based proteasome inhibitor bortezomib in complex with the yeast 20S proteasome., Groll M, Berkers CR, Ploegh HL, Ovaa H, Structure. 2006 Mar;14(3):451-6. PMID:16531229
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