1jd2

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{{STRUCTURE_1jd2| PDB=1jd2 | SCENE= }}
{{STRUCTURE_1jd2| PDB=1jd2 | SCENE= }}
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'''Crystal Structure of the yeast 20S Proteasome:TMC-95A complex: A non-covalent Proteasome Inhibitor'''
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===Crystal Structure of the yeast 20S Proteasome:TMC-95A complex: A non-covalent Proteasome Inhibitor===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 11493007 is the PubMed ID number.
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{{ABSTRACT_PUBMED_11493007}}
==About this Structure==
==About this Structure==
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[[Category: Beta-sandwich]]
[[Category: Beta-sandwich]]
[[Category: Proteasome:inhibitor complex]]
[[Category: Proteasome:inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 21:04:33 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 1 20:03:11 2008''

Revision as of 17:03, 1 July 2008

Image:1jd2.png

Template:STRUCTURE 1jd2

Crystal Structure of the yeast 20S Proteasome:TMC-95A complex: A non-covalent Proteasome Inhibitor

Template:ABSTRACT PUBMED 11493007

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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