1bzy | pdb_00001bzy

HUMAN HGPRTASE WITH TRANSITION STATE INHIBITOR

File:1bzy.gif

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1bzy, resolution 2.00Å (default scene)
Ligands:	IMU, MG, POP
Activity:	Hypoxanthine phosphoribosyltransferase, with EC number 2.4.2.8
Structural annotation: Resources: CATH : 1Bzya00, 1Bzyb00, 1Bzyc00, 1Bzyd00 InterPro : Ipr005904, Ipr002375, Ipr000836 Pfam : PF00156 SCOP : d1bzya_, d1bzyb_, d1bzyc_, d1bzyd_ UniProt : P00492
Functional annotation: Cellular component: cytoplasm Biological process: purine nucleotide biosynthetic process purine ribonucleoside salvage nucleoside metabolic process hypoxanthine metabolic process protein homotetramerization behavior positive regulation of dopamine metabolic process Molecular function: transferase activity, transferring glycosyl groups hypoxanthine phosphoribosyltransferase activity protein binding protein homodimerization activity transferase activity magnesium ion binding metal ion binding
Evolutionary conservation: Toggle Conservation Colors: Rows = identical sequences: Further Information: Caveats, Explanation, Complete Results at ConSurfDB
Resources:	FirstGlance, OCA, RCSB, PDBsum
Coordinates:	save as pdb, mmCIF, xml

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

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