2itk

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{{STRUCTURE_2itk| PDB=2itk | SCENE= }}
{{STRUCTURE_2itk| PDB=2itk | SCENE= }}
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'''human Pin1 bound to D-PEPTIDE'''
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===human Pin1 bound to D-PEPTIDE===
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==Overview==
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Human Pin1 is a key regulator of cell-cycle progression and plays growth-promoting roles in human cancers. High-affinity inhibitors of Pin1 may provide a unique opportunity for disrupting oncogenic pathways. Here we report two high-resolution X-ray crystal structures of human Pin1 bound to non-natural peptide inhibitors. The structures of the bound high-affinity peptides identify a type-I beta-turn conformation for Pin1 prolyl peptide isomerase domain-peptide binding and an extensive molecular interface for high-affinity recognition. Moreover, these structures suggest chemical elements that may further improve the affinity and pharmacological properties of future peptide-based Pin inhibitors. Finally, an intramolecular hydrogen bond observed in both peptide complexes mimics the cyclic conformation of FK506 and rapamycin. Both FK506 and rapamycin are clinically important inhibitors of other peptidyl-prolyl cis-trans isomerases. This comparative discovery suggests that a cyclic peptide polyketide bridge, like that found in FK506 and rapamycin or a similar linkage, may significantly improve the binding affinity of structure-based Pin1 inhibitors.
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(as it appears on PubMed at http://www.pubmed.gov), where 17518432 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17518432}}
==About this Structure==
==About this Structure==
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[[Category: Pin1]]
[[Category: Pin1]]
[[Category: Ww domain]]
[[Category: Ww domain]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu May 22 22:25:10 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 14:32:41 2008''

Revision as of 11:32, 27 July 2008

Image:2itk.png

Template:STRUCTURE 2itk

human Pin1 bound to D-PEPTIDE

Template:ABSTRACT PUBMED 17518432

About this Structure

2ITK is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural basis for high-affinity peptide inhibition of human Pin1., Zhang Y, Daum S, Wildemann D, Zhou XZ, Verdecia MA, Bowman ME, Lucke C, Hunter T, Lu KP, Fischer G, Noel JP, ACS Chem Biol. 2007 May 22;2(5):320-8. PMID:17518432

Page seeded by OCA on Sun Jul 27 14:32:41 2008

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