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1g73

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(New page: 200px<br /> <applet load="1g73" size="450" color="white" frame="true" align="right" spinBox="true" caption="1g73, resolution 2.0&Aring;" /> '''CRYSTAL STRUCTURE OF...)
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[[Image:1g73.gif|left|200px]]<br /><applet load="1g73" size="350" color="white" frame="true" align="right" spinBox="true"
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<applet load="1g73" size="450" color="white" frame="true" align="right" spinBox="true"
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caption="1g73, resolution 2.0&Aring;" />
caption="1g73, resolution 2.0&Aring;" />
'''CRYSTAL STRUCTURE OF SMAC BOUND TO XIAP-BIR3 DOMAIN'''<br />
'''CRYSTAL STRUCTURE OF SMAC BOUND TO XIAP-BIR3 DOMAIN'''<br />
==Overview==
==Overview==
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Apoptosis is an essential process in the development and homeostasis of, all metazoans. The inhibitor-of-apoptosis (IAP) proteins suppress cell, death by inhibiting the activity of caspases; this inhibition is performed, by the zinc-binding BIR domains of the IAP proteins. The mitochondrial, protein Smac/DIABLO promotes apoptosis by eliminating the inhibitory, effect of IAPs through physical interactions. Amino-terminal sequences in, Smac/DIABLO are required for this function, as mutation of the very first, amino acid leads to loss of interaction with IAPs and concomitant loss of, Smac/DIABLO function. Here we report the high-resolution crystal structure, of Smac/DIABLO complexed with the third BIR domain (BIR3) of XIAP. Our, results show that the N-terminal four residues (Ala-Val-Pro-Ile) in, Smac/DIABLO recognize a surface groove on BIR3, with the first residue Ala, binding a hydrophobic pocket and making five hydrogen bonds to, neighbouring residues on BIR3. These observations provide a structural, explanation for the roles of the Smac N terminus as well as the conserved, N-terminal sequences in the Drosophila proteins Hid/Grim/Reaper. In, conjunction with other observations, our results reveal how Smac may, relieve IAP inhibition of caspase-9 activity. In addition to explaining a, number of biological observations, our structural analysis identifies, potential targets for drug screening.
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Apoptosis is an essential process in the development and homeostasis of all metazoans. The inhibitor-of-apoptosis (IAP) proteins suppress cell death by inhibiting the activity of caspases; this inhibition is performed by the zinc-binding BIR domains of the IAP proteins. The mitochondrial protein Smac/DIABLO promotes apoptosis by eliminating the inhibitory effect of IAPs through physical interactions. Amino-terminal sequences in Smac/DIABLO are required for this function, as mutation of the very first amino acid leads to loss of interaction with IAPs and concomitant loss of Smac/DIABLO function. Here we report the high-resolution crystal structure of Smac/DIABLO complexed with the third BIR domain (BIR3) of XIAP. Our results show that the N-terminal four residues (Ala-Val-Pro-Ile) in Smac/DIABLO recognize a surface groove on BIR3, with the first residue Ala binding a hydrophobic pocket and making five hydrogen bonds to neighbouring residues on BIR3. These observations provide a structural explanation for the roles of the Smac N terminus as well as the conserved N-terminal sequences in the Drosophila proteins Hid/Grim/Reaper. In conjunction with other observations, our results reveal how Smac may relieve IAP inhibition of caspase-9 activity. In addition to explaining a number of biological observations, our structural analysis identifies potential targets for drug screening.
==Disease==
==Disease==
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==About this Structure==
==About this Structure==
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1G73 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with ZN as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1G73 OCA].
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1G73 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=ZN:'>ZN</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1G73 OCA].
==Reference==
==Reference==
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[[Category: Chai, J.]]
[[Category: Chai, J.]]
[[Category: Shi, Y.]]
[[Category: Shi, Y.]]
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[[Category: Suber, T.L.]]
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[[Category: Suber, T L.]]
[[Category: Wu, G.]]
[[Category: Wu, G.]]
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[[Category: Wu, J.W.]]
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[[Category: Wu, J W.]]
[[Category: ZN]]
[[Category: ZN]]
[[Category: helix bundle]]
[[Category: helix bundle]]
[[Category: zinc-binding domain]]
[[Category: zinc-binding domain]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 17:01:19 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:46:50 2008''

Revision as of 10:46, 21 February 2008


1g73, resolution 2.0Å

Drag the structure with the mouse to rotate

CRYSTAL STRUCTURE OF SMAC BOUND TO XIAP-BIR3 DOMAIN

Contents

Overview

Apoptosis is an essential process in the development and homeostasis of all metazoans. The inhibitor-of-apoptosis (IAP) proteins suppress cell death by inhibiting the activity of caspases; this inhibition is performed by the zinc-binding BIR domains of the IAP proteins. The mitochondrial protein Smac/DIABLO promotes apoptosis by eliminating the inhibitory effect of IAPs through physical interactions. Amino-terminal sequences in Smac/DIABLO are required for this function, as mutation of the very first amino acid leads to loss of interaction with IAPs and concomitant loss of Smac/DIABLO function. Here we report the high-resolution crystal structure of Smac/DIABLO complexed with the third BIR domain (BIR3) of XIAP. Our results show that the N-terminal four residues (Ala-Val-Pro-Ile) in Smac/DIABLO recognize a surface groove on BIR3, with the first residue Ala binding a hydrophobic pocket and making five hydrogen bonds to neighbouring residues on BIR3. These observations provide a structural explanation for the roles of the Smac N terminus as well as the conserved N-terminal sequences in the Drosophila proteins Hid/Grim/Reaper. In conjunction with other observations, our results reveal how Smac may relieve IAP inhibition of caspase-9 activity. In addition to explaining a number of biological observations, our structural analysis identifies potential targets for drug screening.

Disease

Known diseases associated with this structure: Lymphoproliferative syndrome, X-linked, 2 OMIM:[300079]

About this Structure

1G73 is a Protein complex structure of sequences from Homo sapiens with as ligand. Full crystallographic information is available from OCA.

Reference

Structural basis of IAP recognition by Smac/DIABLO., Wu G, Chai J, Suber TL, Wu JW, Du C, Wang X, Shi Y, Nature. 2000 Dec 21-28;408(6815):1008-12. PMID:11140638

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