1xoi
From Proteopedia
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|PDB= 1xoi |SIZE=350|CAPTION= <scene name='initialview01'>1xoi</scene>, resolution 2.1Å | |PDB= 1xoi |SIZE=350|CAPTION= <scene name='initialview01'>1xoi</scene>, resolution 2.1Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= <scene name='pdbligand=NBG:1-N-ACETYL-BETA-D-GLUCOSAMINE'>NBG</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5'-PHOSPHATE'>PLP</scene> | + | |LIGAND= <scene name='pdbligand=288:5-CHLORO-1H-INDOLE-2-CARBOXYLIC+ACID{[CYCLOPENTYL-(2-HYDROXY-ETHYL)-CARBAMOYL]-METHYL}-AMIDE'>288</scene>, <scene name='pdbligand=NBG:1-N-ACETYL-BETA-D-GLUCOSAMINE'>NBG</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5'-PHOSPHATE'>PLP</scene> |
| - | + | |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> | |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1em6|1EM6]], [[1exv|1EXV]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1xoi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1xoi OCA], [http://www.ebi.ac.uk/pdbsum/1xoi PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1xoi RCSB]</span> | ||
}} | }} | ||
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==Overview== | ==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. | 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:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=232700 232700]] | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Treadway, J L.]] | [[Category: Treadway, J L.]] | ||
[[Category: Wright, S W.]] | [[Category: Wright, S W.]] | ||
| - | [[Category: 288]] | ||
| - | [[Category: NBG]] | ||
| - | [[Category: PLP]] | ||
[[Category: allosteric enzyme]] | [[Category: allosteric enzyme]] | ||
[[Category: glycogen storage disease]] | [[Category: glycogen storage disease]] | ||
[[Category: glycosyltransferase]] | [[Category: glycosyltransferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:52:27 2008'' |
Revision as of 21:52, 30 March 2008
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| , resolution 2.1Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , | ||||||
| Activity: | Phosphorylase, with EC number 2.4.1.1 | ||||||
| Related: | 1EM6, 1EXV
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Human Liver Glycogen Phosphorylase A complexed with Chloroindoloyl glycine amide
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.
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
Page seeded by OCA on Mon Mar 31 00:52:27 2008
