2f16
From Proteopedia
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| - | [[Image:2f16.gif|left|200px]] | + | [[Image:2f16.gif|left|200px]] |
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| - | '''Crystal structure of the yeast 20S proteasome in complex with bortezomib''' | + | {{Structure |
| + | |PDB= 2f16 |SIZE=350|CAPTION= <scene name='initialview01'>2f16</scene>, resolution 2.8Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=BO2:N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE'>BO2</scene> | ||
| + | |ACTIVITY= [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] | ||
| + | |GENE= | ||
| + | }} | ||
| + | |||
| + | '''Crystal structure of the yeast 20S proteasome in complex with bortezomib''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2F16 is a [ | + | 2F16 is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2F16 OCA]. |
==Reference== | ==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:[http:// | + | 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:[http://www.ncbi.nlm.nih.gov/pubmed/16531229 16531229] |
[[Category: Proteasome endopeptidase complex]] | [[Category: Proteasome endopeptidase complex]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
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[[Category: Groll, M.]] | [[Category: Groll, M.]] | ||
[[Category: BO2]] | [[Category: BO2]] | ||
| - | [[Category: beta-sandwich flanked by | + | [[Category: beta-sandwich flanked by helice]] |
[[Category: complex structure covalently bound to the synthetic inihibtor bortezomib]] | [[Category: complex structure covalently bound to the synthetic inihibtor bortezomib]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:46:49 2008'' |
Revision as of 14:46, 20 March 2008
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| , resolution 2.8Å | |||||||
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| Ligands: | |||||||
| Activity: | Proteasome endopeptidase complex, with EC number 3.4.25.1 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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
Page seeded by OCA on Thu Mar 20 16:46:49 2008
