1xoi: Difference between revisions
New page: left|200px<br /> <applet load="1xoi" size="450" color="white" frame="true" align="right" spinBox="true" caption="1xoi, resolution 2.1Å" /> '''Human Liver Glycogen... |
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[[Image:1xoi.gif|left|200px]]<br /> | [[Image:1xoi.gif|left|200px]]<br /><applet load="1xoi" size="350" color="white" frame="true" align="right" spinBox="true" | ||
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caption="1xoi, resolution 2.1Å" /> | caption="1xoi, resolution 2.1Å" /> | ||
'''Human Liver Glycogen Phosphorylase A complexed with Chloroindoloyl glycine amide'''<br /> | '''Human Liver Glycogen Phosphorylase A complexed with Chloroindoloyl glycine amide'''<br /> | ||
==Overview== | ==Overview== | ||
The synthesis, in vitro, and in vivo biological characterization of a | 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== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
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 NBG, PLP and 288 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:// | 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]. | ||
==Reference== | ==Reference== | ||
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[[Category: Phosphorylase]] | [[Category: Phosphorylase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Gibbs, E | [[Category: Gibbs, E M.]] | ||
[[Category: Rath, V | [[Category: Rath, V L.]] | ||
[[Category: Treadway, J | [[Category: Treadway, J L.]] | ||
[[Category: Wright, S | [[Category: Wright, S W.]] | ||
[[Category: 288]] | [[Category: 288]] | ||
[[Category: NBG]] | [[Category: NBG]] | ||
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[[Category: glycosyltransferase]] | [[Category: glycosyltransferase]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:56:57 2008'' | ||
Revision as of 16:57, 21 February 2008
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Human Liver Glycogen Phosphorylase A complexed with Chloroindoloyl glycine amide
OverviewOverview
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.
DiseaseDisease
Known disease associated with this structure: Glycogen storage disease VI OMIM:[232700]
About this StructureAbout this Structure
1XOI is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Phosphorylase, with EC number 2.4.1.1 Full crystallographic information is available from OCA.
ReferenceReference
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
Page seeded by OCA on Thu Feb 21 15:56:57 2008