1hlf

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[[Image:1hlf.gif|left|200px]]
[[Image:1hlf.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1hlf |SIZE=350|CAPTION= <scene name='initialview01'>1hlf</scene>, resolution 2.26&Aring;
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The line below this paragraph, containing "STRUCTURE_1hlf", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=GL4:8,9,10-TRIHYDROXY-7-HYDROXYMETHYL-2-THIOXO-6-OXA-1,3-DIAZA-SPIRO[4.5]DECAN-4-ONE'>GL4</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5&#39;-PHOSPHATE'>PLP</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphorylase Phosphorylase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.4.1.1 2.4.1.1] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1hlf| PDB=1hlf | SCENE= }}
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|RELATEDENTRY=[[1ggn|1GGN]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1hlf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1hlf OCA], [http://www.ebi.ac.uk/pdbsum/1hlf PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1hlf RCSB]</span>
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}}
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'''BINDING OF GLUCOPYRANOSYLIDENE-SPIRO-THIOHYDANTOIN TO GLYCOGEN PHOSPHORYLASE B: KINETIC AND CRYSTALLOGRAPHIC STUD'''
'''BINDING OF GLUCOPYRANOSYLIDENE-SPIRO-THIOHYDANTOIN TO GLYCOGEN PHOSPHORYLASE B: KINETIC AND CRYSTALLOGRAPHIC STUD'''
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[[Category: Szilagyi, L.]]
[[Category: Szilagyi, L.]]
[[Category: Toth, B.]]
[[Category: Toth, B.]]
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[[Category: catalytic site]]
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[[Category: Catalytic site]]
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[[Category: design]]
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[[Category: Design]]
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[[Category: glycogen phosphorylase]]
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[[Category: Glycogen phosphorylase]]
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[[Category: inhibitor complex]]
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[[Category: Inhibitor complex]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 18:58:53 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:07:13 2008''
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Revision as of 15:58, 2 May 2008

Image:1hlf.gif

Template:STRUCTURE 1hlf

BINDING OF GLUCOPYRANOSYLIDENE-SPIRO-THIOHYDANTOIN TO GLYCOGEN PHOSPHORYLASE B: KINETIC AND CRYSTALLOGRAPHIC STUD


Overview

Glucopyranosylidene spirothiohydantoin (TH) has been identified as a potential inhibitor of both muscle and liver glycogen phosphorylase b (GPb) and a (GPa) and shown to diminish liver GPa activity in vitro. Kinetic experiments reported here show that TH inhibits muscle GPb competitively with respect to both substrates phosphate (K(i)=2.3 microM) and glycogen (K(i)=2.8 microM). The structure of the GPb-TH complex has been determined at a resolution of 2.26 A and refined to a crystallographic R value of 0.193 (R(free)=0.211). The structure of GPb-TH complex reveals that the inhibitor can be accommodated in the catalytic site of T-state GPb with very little change of the tertiary structure, and provides a basis of understanding potency and specificity of the inhibitor. The glucopyranose moiety makes the standard hydrogen bonds and van der Waals contacts as observed in the glucose complex, while the rigid thiohydantoin group is in a favourable electrostatic environment and makes additional polar contacts to the protein.

About this Structure

1HLF is a Single protein structure of sequence from Oryctolagus cuniculus. Full crystallographic information is available from OCA.

Reference

Kinetic and crystallographic studies of glucopyranosylidene spirothiohydantoin binding to glycogen phosphorylase B., Oikonomakos NG, Skamnaki VT, Osz E, Szilagyi L, Somsak L, Docsa T, Toth B, Gergely P, Bioorg Med Chem. 2002 Feb;10(2):261-8. PMID:11741774 Page seeded by OCA on Fri May 2 18:58:53 2008

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