2vge

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[[Image:2vge.jpg|left|200px]]
[[Image:2vge.jpg|left|200px]]
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{{Structure
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{{STRUCTURE_2vge| PDB=2vge | SCENE= }}
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2vge FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2vge OCA], [http://www.ebi.ac.uk/pdbsum/2vge PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2vge RCSB]</span>
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'''CRYSTAL STRUCTURE OF THE C-TERMINAL REGION OF HUMAN IASPP'''
'''CRYSTAL STRUCTURE OF THE C-TERMINAL REGION OF HUMAN IASPP'''
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[[Category: Robinson, R A.]]
[[Category: Robinson, R A.]]
[[Category: Siebold, C.]]
[[Category: Siebold, C.]]
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[[Category: alternative splicing]]
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[[Category: Alternative splicing]]
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[[Category: ank repeat]]
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[[Category: Ank repeat]]
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[[Category: ankyrin repeat]]
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[[Category: Ankyrin repeat]]
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[[Category: apoptosis]]
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[[Category: Apoptosis]]
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[[Category: cytoplasm]]
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[[Category: Cytoplasm]]
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[[Category: iaspp]]
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[[Category: Iaspp]]
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[[Category: nucleus]]
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[[Category: Nucleus]]
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[[Category: p53 binding protein]]
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[[Category: P53 binding protein]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: repressor]]
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[[Category: Repressor]]
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[[Category: sh3 domain]]
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[[Category: Sh3 domain]]
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[[Category: transcription]]
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[[Category: Transcription]]
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[[Category: transcription regulation]]
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[[Category: Transcription regulation]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 18:45:25 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:11:54 2008''
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Revision as of 15:45, 4 May 2008

Template:STRUCTURE 2vge

CRYSTAL STRUCTURE OF THE C-TERMINAL REGION OF HUMAN IASPP


Overview

ASPP1 and ASPP2 are activators of p53-dependent apoptosis, whereas iASPP is an inhibitor of p53. Binding assays showed differential binding for C-terminal domains of iASPP and ASPP2 to the core domains of p53 family members p53, p63, and p73. We also determined a high-resolution crystal structure for the C terminus of iASPP, comprised of four ankyrin repeats and an SH3 domain. The crystal lattice revealed an interaction between eight sequential residues in one iASPP molecule and the p53-binding site of a neighboring molecule. ITC confirmed that a peptide corresponding to the crystallographic interaction shows specific binding to iASPP. The contributions of ankyrin repeat residues, in addition to those of the SH3 domain, generate distinctive architecture at the p53-binding site suitable for inhibition by small molecules. These results suggest that the binding properties of iASPP render it a target for antitumor therapeutics and provide a peptide-based template for compound design.

About this Structure

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

Reference

Biochemical and Structural Studies of ASPP Proteins Reveal Differential Binding to p53, p63, and p73., Robinson RA, Lu X, Jones EY, Siebold C, Structure. 2008 Feb;16(2):259-68. PMID:18275817 Page seeded by OCA on Sun May 4 18:45:25 2008

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