1xoi

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[[Image:1xoi.gif|left|200px]]<br /><applet load="1xoi" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1xoi.gif|left|200px]]
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caption="1xoi, resolution 2.1&Aring;" />
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'''Human Liver Glycogen Phosphorylase A complexed with Chloroindoloyl glycine amide'''<br />
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{{Structure
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|PDB= 1xoi |SIZE=350|CAPTION= <scene name='initialview01'>1xoi</scene>, resolution 2.1&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=NBG:1-N-ACETYL-BETA-D-GLUCOSAMINE'>NBG</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5'-PHOSPHATE'>PLP</scene> and <scene name='pdbligand=288:5-CHLORO-1H-INDOLE-2-CARBOXYLIC ACID{[CYCLOPENTYL-(2-HYDROXY-ETHYL)-CARBAMOYL]-METHYL}-AMIDE'>288</scene>
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|ACTIVITY= [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]
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|GENE=
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}}
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'''Human Liver Glycogen Phosphorylase A complexed with Chloroindoloyl glycine amide'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1XOI 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=NBG:'>NBG</scene>, <scene name='pdbligand=PLP:'>PLP</scene> and <scene name='pdbligand=288:'>288</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XOI OCA].
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1XOI is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XOI OCA].
==Reference==
==Reference==
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5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization., Wright SW, Rath VL, Genereux PE, Hageman DL, Levy CB, McClure LD, McCoid SC, McPherson RK, Schelhorn TM, Wilder DE, Zavadoski WJ, Gibbs EM, Treadway JL, Bioorg Med Chem Lett. 2005 Jan 17;15(2):459-65. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15603973 15603973]
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5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization., Wright SW, Rath VL, Genereux PE, Hageman DL, Levy CB, McClure LD, McCoid SC, McPherson RK, Schelhorn TM, Wilder DE, Zavadoski WJ, Gibbs EM, Treadway JL, Bioorg Med Chem Lett. 2005 Jan 17;15(2):459-65. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15603973 15603973]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Phosphorylase]]
[[Category: Phosphorylase]]
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[[Category: glycosyltransferase]]
[[Category: glycosyltransferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:56:57 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:12:31 2008''

Revision as of 13:12, 20 March 2008


PDB ID 1xoi

Drag the structure with the mouse to rotate
, resolution 2.1Å
Ligands: , and
Activity: Phosphorylase, with EC number 2.4.1.1
Coordinates: save as pdb, mmCIF, xml



Human Liver Glycogen Phosphorylase A complexed with Chloroindoloyl glycine amide


Contents

Overview

The synthesis, in vitro, and in vivo biological characterization of a series of achiral 5-chloroindoloyl glycine amide inhibitors of human liver glycogen phosphorylase A are described. Improved potency over previously reported compounds in cellular and in vivo assays was observed. The allosteric binding site of these compounds was shown by X-ray crystallography to be the same as that reported previously for 5-chloroindoloyl norstatine amides.

Disease

Known disease associated with this structure: Glycogen storage disease VI OMIM:[232700]

About this Structure

1XOI is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization., Wright SW, Rath VL, Genereux PE, Hageman DL, Levy CB, McClure LD, McCoid SC, McPherson RK, Schelhorn TM, Wilder DE, Zavadoski WJ, Gibbs EM, Treadway JL, Bioorg Med Chem Lett. 2005 Jan 17;15(2):459-65. PMID:15603973

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