1bzy
From Proteopedia
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[[Image:1bzy.gif|left|200px]] | [[Image:1bzy.gif|left|200px]] | ||
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'''HUMAN HGPRTASE WITH TRANSITION STATE INHIBITOR''' | '''HUMAN HGPRTASE WITH TRANSITION STATE INHIBITOR''' | ||
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[[Category: Shi, W.]] | [[Category: Shi, W.]] | ||
[[Category: Tyler, P C.]] | [[Category: Tyler, P C.]] | ||
- | [[Category: | + | [[Category: Hgprt]] |
- | [[Category: | + | [[Category: Immucillin]] |
- | [[Category: | + | [[Category: Lesch-nyhan]] |
- | [[Category: | + | [[Category: Magnesium]] |
- | [[Category: | + | [[Category: Neighboring group participation]] |
- | [[Category: | + | [[Category: Oxocarbenium ion]] |
- | [[Category: | + | [[Category: Phosphoribosyltransferase]] |
- | [[Category: | + | [[Category: Pyrophosphate]] |
- | [[Category: | + | [[Category: Transition state]] |
- | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 12:10:06 2008'' | |
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + |
Revision as of 09:10, 2 May 2008
HUMAN HGPRTASE WITH TRANSITION STATE INHIBITOR
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.
About this Structure
1BZY is a Single protein structure of sequence from Homo sapiens. 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 Fri May 2 12:10:06 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. | Hgprt | Immucillin | Lesch-nyhan | Magnesium | Neighboring group participation | Oxocarbenium ion | Phosphoribosyltransferase | Pyrophosphate | Transition state