1bzy
From Proteopedia
(New page: 200px<br /> <applet load="1bzy" size="450" color="white" frame="true" align="right" spinBox="true" caption="1bzy, resolution 2.00Å" /> '''HUMAN HGPRTASE WITH...) |
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| - | [[Image:1bzy.gif|left|200px]]<br /> | + | [[Image:1bzy.gif|left|200px]]<br /><applet load="1bzy" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1bzy" size=" | + | |
caption="1bzy, resolution 2.00Å" /> | caption="1bzy, resolution 2.00Å" /> | ||
'''HUMAN HGPRTASE WITH TRANSITION STATE INHIBITOR'''<br /> | '''HUMAN HGPRTASE WITH TRANSITION STATE INHIBITOR'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The structure of human HGPRT bound to the transition-state analog | + | The structure of human HGPRT bound to the transition-state analog immucillinGP and Mg2+-pyrophosphate has been determined to 2.0 A resolution. ImmucillinGP was designed as a stable analog with the stereoelectronic features of the transition state. Bound inhibitor at the catalytic site indicates that the oxocarbenium ion of the transition state is stabilized by neighboring-group participation from MgPPi and O5'. A short hydrogen bond forms between Asp 137 and the purine ring analog. Two Mg2+ ions sandwich the pyrophosphate and contact both hydroxyls of the ribosyl analog. The transition-state analog is shielded from bulk solvent by a catalytic loop that moves approximately 25 A to cover the active site and becomes an ordered antiparallel beta-sheet. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1BZY 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 MG, IMU and POP as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Hypoxanthine_phosphoribosyltransferase Hypoxanthine phosphoribosyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.8 2.4.2.8] Full crystallographic information is available from [http:// | + | 1BZY 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=MG:'>MG</scene>, <scene name='pdbligand=IMU:'>IMU</scene> and <scene name='pdbligand=POP:'>POP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Hypoxanthine_phosphoribosyltransferase Hypoxanthine phosphoribosyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.2.8 2.4.2.8] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1BZY OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Hypoxanthine phosphoribosyltransferase]] | [[Category: Hypoxanthine phosphoribosyltransferase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Almo, S | + | [[Category: Almo, S C.]] |
| - | [[Category: Furneaux, R | + | [[Category: Furneaux, R H.]] |
[[Category: Grubmeyer, C.]] | [[Category: Grubmeyer, C.]] | ||
[[Category: Li, C.]] | [[Category: Li, C.]] | ||
| - | [[Category: Schramm, V | + | [[Category: Schramm, V L.]] |
[[Category: Shi, W.]] | [[Category: Shi, W.]] | ||
| - | [[Category: Tyler, P | + | [[Category: Tyler, P C.]] |
[[Category: IMU]] | [[Category: IMU]] | ||
[[Category: MG]] | [[Category: MG]] | ||
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[[Category: transition state]] | [[Category: transition state]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:00:59 2008'' |
Revision as of 10:01, 21 February 2008
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HUMAN HGPRTASE WITH TRANSITION STATE INHIBITOR
Contents |
Overview
The structure of human HGPRT bound to the transition-state analog immucillinGP and Mg2+-pyrophosphate has been determined to 2.0 A resolution. ImmucillinGP was designed as a stable analog with the stereoelectronic features of the transition state. Bound inhibitor at the catalytic site indicates that the oxocarbenium ion of the transition state is stabilized by neighboring-group participation from MgPPi and O5'. A short hydrogen bond forms between Asp 137 and the purine ring analog. Two Mg2+ ions sandwich the pyrophosphate and contact both hydroxyls of the ribosyl analog. The transition-state analog is shielded from bulk solvent by a catalytic loop that moves approximately 25 A to cover the active site and becomes an ordered antiparallel beta-sheet.
Disease
Known diseases associated with this structure: HPRT-related gout OMIM:[308000], Lesch-Nyhan syndrome, 300322, OMIM:[308000]
About this Structure
1BZY is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Hypoxanthine phosphoribosyltransferase, with EC number 2.4.2.8 Full crystallographic information is available from OCA.
Reference
The 2.0 A structure of human hypoxanthine-guanine phosphoribosyltransferase in complex with a transition-state analog inhibitor., Shi W, Li CM, Tyler PC, Furneaux RH, Grubmeyer C, Schramm VL, Almo SC, Nat Struct Biol. 1999 Jun;6(6):588-93. PMID:10360366
Page seeded by OCA on Thu Feb 21 12:00:59 2008
Categories: Homo sapiens | Hypoxanthine phosphoribosyltransferase | Single protein | Almo, S C. | Furneaux, R H. | Grubmeyer, C. | Li, C. | Schramm, V L. | Shi, W. | Tyler, P C. | IMU | MG | POP | Hgprt | Immucillin | Lesch-nyhan | Magnesium | Neighboring group participation | Oxocarbenium ion | Phosphoribosyltransferase | Pyrophosphate | Transition state
