2opy
From Proteopedia
(New page: 200px<br /> <applet load="2opy" size="450" color="white" frame="true" align="right" spinBox="true" caption="2opy, resolution 2.8Å" /> '''Smac mimic bound to ...) |
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| - | [[Image:2opy.gif|left|200px]]<br /> | + | [[Image:2opy.gif|left|200px]]<br /><applet load="2opy" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2opy" size=" | + | |
caption="2opy, resolution 2.8Å" /> | caption="2opy, resolution 2.8Å" /> | ||
'''Smac mimic bound to BIR3-XIAP'''<br /> | '''Smac mimic bound to BIR3-XIAP'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A small series of peptide mimics was designed and synthesized to contain a | + | A small series of peptide mimics was designed and synthesized to contain a heterocyclic ring in place of the potentially labile N-terminal peptide bond of the tetrapeptide containing the Smac-XIAP-binding motif. Two Smac mimics were shown to bind to the BIR3 domain of XIAP with moderate affinity and one displayed increased activity in cells relative to the Smac peptides. The structures of BIR3-XIAP in complex with a Smac peptide and a peptide mimic were solved and analyzed to elucidate the structure-activity relationship surrounding the Smac-binding domain within BIR3-XIAP. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2OPY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with ZN and CO9 as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 2OPY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=ZN:'>ZN</scene> and <scene name='pdbligand=CO9:'>CO9</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2OPY OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Lu, G.]] | [[Category: Lu, G.]] | ||
| - | [[Category: McLendon, G | + | [[Category: McLendon, G L.]] |
| - | [[Category: Riedl, S | + | [[Category: Riedl, S J.]] |
[[Category: Shi, Y.]] | [[Category: Shi, Y.]] | ||
| - | [[Category: Wist, A | + | [[Category: Wist, A D.]] |
[[Category: CO9]] | [[Category: CO9]] | ||
[[Category: ZN]] | [[Category: ZN]] | ||
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[[Category: peptide mimic]] | [[Category: peptide mimic]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:21:14 2008'' |
Revision as of 16:21, 21 February 2008
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Smac mimic bound to BIR3-XIAP
Contents |
Overview
A small series of peptide mimics was designed and synthesized to contain a heterocyclic ring in place of the potentially labile N-terminal peptide bond of the tetrapeptide containing the Smac-XIAP-binding motif. Two Smac mimics were shown to bind to the BIR3 domain of XIAP with moderate affinity and one displayed increased activity in cells relative to the Smac peptides. The structures of BIR3-XIAP in complex with a Smac peptide and a peptide mimic were solved and analyzed to elucidate the structure-activity relationship surrounding the Smac-binding domain within BIR3-XIAP.
Disease
Known diseases associated with this structure: Lymphoproliferative syndrome, X-linked, 2 OMIM:[300079]
About this Structure
2OPY is a Single protein structure of sequence from Homo sapiens with and as ligands. Full crystallographic information is available from OCA.
Reference
Structure-activity based study of the Smac-binding pocket within the BIR3 domain of XIAP., Wist AD, Gu L, Riedl SJ, Shi Y, McLendon GL, Bioorg Med Chem. 2007 Apr 15;15(8):2935-43. Epub 2007 Feb 11. PMID:17336535
Page seeded by OCA on Thu Feb 21 18:21:14 2008
Categories: Homo sapiens | Single protein | Lu, G. | McLendon, G L. | Riedl, S J. | Shi, Y. | Wist, A D. | CO9 | ZN | Bir3 | Peptide mimic
