2gpl

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{{STRUCTURE_2gpl| PDB=2gpl | SCENE= }}
{{STRUCTURE_2gpl| PDB=2gpl | SCENE= }}
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'''TMC-95 based biphenyl-ether macrocycles: specific proteasome inhibitors'''
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===TMC-95 based biphenyl-ether macrocycles: specific proteasome inhibitors===
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==Overview==
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TMC-95's natural cyclic tripeptide metabolites represent potent competitive proteasome inhibitors. The constrained conformation of TMC-95 proteasomal inhibitors provides the driving force for entropically high-affinity binding. Based on the crystal structure of the proteasome:TMC-95A complex, the synthetically challenging TMC-95 core structure was used for the design and synthesis of less demanding biphenyl-ether macrocycles, in which the biphenyl-ether moiety functions as an endocyclic clamp restricting its tripeptide backbone. These simplified analogs allowed us to identify high plasticity of the proteasomal tryptic-like specificity pocket. Biphenyl-ether compounds extended with an amide group were hydrolyzed by the proteasome, although the crystal structure of such proteasome:biphenyl-ether complexes revealed quenching of proteolysis at the acyl-enzyme intermediate. Our data reveal that biphenyl-ether derivatives bind noncovalently to the proteasomal tryptic-like active site in a reversible substrate-like manner without allosteric changes of active site residues.
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==About this Structure==
==About this Structure==
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[[Category: Ntn-hydrolase]]
[[Category: Ntn-hydrolase]]
[[Category: Proteasomal subunit fold represents an antiparallel beta-sheet flanked by helice]]
[[Category: Proteasomal subunit fold represents an antiparallel beta-sheet flanked by helice]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:22:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 20:53:02 2008''

Revision as of 17:53, 27 July 2008

Image:2gpl.png

Template:STRUCTURE 2gpl

TMC-95 based biphenyl-ether macrocycles: specific proteasome inhibitors

Template:ABSTRACT PUBMED 16793518

About this Structure

2GPL is a Protein complex structure of sequences from Saccharomyces cerevisiae. Full crystallographic information is available from OCA.

Reference

TMC-95-based inhibitor design provides evidence for the catalytic versatility of the proteasome., Groll M, Gotz M, Kaiser M, Weyher E, Moroder L, Chem Biol. 2006 Jun;13(6):607-14. PMID:16793518

Page seeded by OCA on Sun Jul 27 20:53:02 2008

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