2f16

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[[Image:2f16.gif|left|200px]]
[[Image:2f16.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2f16 |SIZE=350|CAPTION= <scene name='initialview01'>2f16</scene>, resolution 2.8&Aring;
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The line below this paragraph, containing "STRUCTURE_2f16", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=BO2:N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE'>BO2</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2f16| PDB=2f16 | SCENE= }}
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|RELATEDENTRY=[[1ryp|1RYP]], [[1pma|1PMA]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2f16 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2f16 OCA], [http://www.ebi.ac.uk/pdbsum/2f16 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2f16 RCSB]</span>
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}}
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'''Crystal structure of the yeast 20S proteasome in complex with bortezomib'''
'''Crystal structure of the yeast 20S proteasome in complex with bortezomib'''
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[[Category: Saccharomyces cerevisiae]]
[[Category: Saccharomyces cerevisiae]]
[[Category: Groll, M.]]
[[Category: Groll, M.]]
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[[Category: beta-sandwich flanked by helice]]
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[[Category: Beta-sandwich flanked by helice]]
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[[Category: complex structure covalently bound to the synthetic inihibtor bortezomib]]
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[[Category: Complex structure covalently bound to the synthetic inihibtor bortezomib]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:20:29 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:56:35 2008''
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Revision as of 00:20, 4 May 2008

Image:2f16.gif

Template:STRUCTURE 2f16

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 Sun May 4 03:20:29 2008

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OCA

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