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1jd2
From Proteopedia
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|PDB= 1jd2 |SIZE=350|CAPTION= <scene name='initialview01'>1jd2</scene>, resolution 3.0Å | |PDB= 1jd2 |SIZE=350|CAPTION= <scene name='initialview01'>1jd2</scene>, resolution 3.0Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand= | + | |LIGAND= <scene name='pdbligand=95A:TMC-95A'>95A</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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] | + | |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> |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1ryp|1RYP]], [[1g0u|1G0U]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1jd2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1jd2 OCA], [http://www.ebi.ac.uk/pdbsum/1jd2 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1jd2 RCSB]</span> | ||
}} | }} | ||
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[[Category: Koguchi, Y.]] | [[Category: Koguchi, Y.]] | ||
[[Category: Kohno, J.]] | [[Category: Kohno, J.]] | ||
| - | [[Category: 95A]] | ||
| - | [[Category: MG]] | ||
[[Category: beta-sandwich]] | [[Category: beta-sandwich]] | ||
[[Category: proteasome:inhibitor complex]] | [[Category: proteasome:inhibitor complex]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:31:55 2008'' |
Revision as of 18:31, 30 March 2008
| |||||||
| , resolution 3.0Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , | ||||||
| Activity: | Proteasome endopeptidase complex, with EC number 3.4.25.1 | ||||||
| Related: | 1RYP, 1G0U
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Crystal Structure of the yeast 20S Proteasome:TMC-95A complex: A non-covalent Proteasome Inhibitor
Overview
The 20 S proteasome core particle (CP), a multicatalytic protease, is involved in a variety of biologically important processes, including immune response, cell-cycle control, metabolic adaptation, stress response and cell differentiation. Therefore, selective inhibition of the CP will be one possible way to influence these essential pathways. Recently, a new class of specific proteasome inhibitors, TMC-95s, was investigated and we now present a biochemical and crystallographic characterisation of the yeast proteasome core particle in complex with the natural product TMC-95A. This unusual heterocyclic compound specifically blocks the active sites of CPs non-covalently, without modifying the nucleophilic Thr1 residue. The inhibitor is bound to the CP by specific hydrogen bonds with the main-chain atoms of the protein. Analysis of the crystal structure of the complex has revealed which portions of TMC-95s are essential for binding to the proteasome. This will form the basis for the development of synthetic selective proteasome inhibitors as promising candidates for anti-tumoral or anti-inflammatory drugs.
About this Structure
1JD2 is a Protein complex structure of sequences from Saccharomyces cerevisiae. Full crystallographic information is available from OCA.
Reference
Crystal structure of the 20 S proteasome:TMC-95A complex: a non-covalent proteasome inhibitor., Groll M, Koguchi Y, Huber R, Kohno J, J Mol Biol. 2001 Aug 17;311(3):543-8. PMID:11493007
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