2f16
From Proteopedia
(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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| - | [[Image:2f16.gif|left|200px]]<br /><applet load="2f16" size=" | + | [[Image:2f16.gif|left|200px]]<br /><applet load="2f16" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2f16, resolution 2.8Å" /> | caption="2f16, resolution 2.8Å" /> | ||
'''Crystal structure of the yeast 20S proteasome in complex with bortezomib'''<br /> | '''Crystal structure of the yeast 20S proteasome in complex with bortezomib'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The dipeptide boronic acid bortezomib, also termed VELCADE, is a | + | 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== | ==About this Structure== | ||
| - | 2F16 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae] with BO2 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Proteasome_endopeptidase_complex Proteasome endopeptidase complex], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.25.1 3.4.25.1] Full crystallographic information is available from [http:// | + | 2F16 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae] with <scene name='pdbligand=BO2:'>BO2</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Proteasome_endopeptidase_complex Proteasome endopeptidase complex], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.25.1 3.4.25.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2F16 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: complex structure covalently bound to the synthetic inihibtor bortezomib]] | [[Category: complex structure covalently bound to the synthetic inihibtor bortezomib]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:16:38 2008'' |
Revision as of 15:16, 21 February 2008
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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 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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