2gm9: Difference between revisions

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[[Image:2gm9.jpg|left|200px]]<br /><applet load="2gm9" size="350" color="white" frame="true" align="right" spinBox="true"
caption="2gm9, resolution 2.30&Aring;" />
'''Structure of rabbit muscle glycogen phosphorylase in complex with thienopyrrole'''<br />


==Overview==
==Structure of rabbit muscle glycogen phosphorylase in complex with thienopyrrole==
Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography.
<StructureSection load='2gm9' size='340' side='right'caption='[[2gm9]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[2gm9]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GM9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2GM9 FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.3&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3TH:2-CHLORO-N-[(3R)-2-OXO-1,2,3,4-TETRAHYDROQUINOLIN-3-YL]-6H-THIENO[2,3-B]PYRROLE-5-CARBOXAMIDE'>3TH</scene>, <scene name='pdbligand=PLR:(5-HYDROXY-4,6-DIMETHYLPYRIDIN-3-YL)METHYL+DIHYDROGEN+PHOSPHATE'>PLR</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2gm9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2gm9 OCA], [https://pdbe.org/2gm9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2gm9 RCSB], [https://www.ebi.ac.uk/pdbsum/2gm9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2gm9 ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/PYGM_RABIT PYGM_RABIT] Phosphorylase is an important allosteric enzyme in carbohydrate metabolism. Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known phosphorylases share catalytic and structural properties.
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/gm/2gm9_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2gm9 ConSurf].
<div style="clear:both"></div>


==About this Structure==
==See Also==
2GM9 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus] with <scene name='pdbligand=PLR:'>PLR</scene> and <scene name='pdbligand=3TH:'>3TH</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=2GM9 OCA].
*[[Glycogen phosphorylase 3D structures|Glycogen phosphorylase 3D structures]]
 
__TOC__
==Reference==
</StructureSection>
Novel thienopyrrole glycogen phosphorylase inhibitors: synthesis, in vitro SAR and crystallographic studies., Whittamore PR, Addie MS, Bennett SN, Birch AM, Butters M, Godfrey L, Kenny PW, Morley AD, Murray PM, Oikonomakos NG, Otterbein LR, Pannifer AD, Parker JS, Readman K, Siedlecki PS, Schofield P, Stocker A, Taylor MJ, Townsend LA, Whalley DP, Whitehouse J, Bioorg Med Chem Lett. 2006 Nov 1;16(21):5567-71. Epub 2006 Aug 30. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16945526 16945526]
[[Category: Large Structures]]
[[Category: Oryctolagus cuniculus]]
[[Category: Oryctolagus cuniculus]]
[[Category: Phosphorylase]]
[[Category: Breed J]]
[[Category: Single protein]]
[[Category: Minshull C]]
[[Category: Breed, J.]]
[[Category: Oikonomakos NG]]
[[Category: Minshull, C.]]
[[Category: Otterbein LR]]
[[Category: Oikonomakos, N G.]]
[[Category: Pannifer AD]]
[[Category: Otterbein, L R.]]
[[Category: Pauptit RA]]
[[Category: Pannifer, A D.]]
[[Category: Rowsell S]]
[[Category: Pauptit, R A.]]
[[Category: Tucker J]]
[[Category: Rowsell, S.]]
[[Category: Tucker, J.]]
[[Category: 3TH]]
[[Category: PLR]]
[[Category: glycogen phosphorylase]]
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:33:04 2008''

Latest revision as of 12:28, 14 February 2024

Structure of rabbit muscle glycogen phosphorylase in complex with thienopyrroleStructure of rabbit muscle glycogen phosphorylase in complex with thienopyrrole

Structural highlights

2gm9 is a 1 chain structure with sequence from Oryctolagus cuniculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 2.3Å
Ligands:,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

PYGM_RABIT Phosphorylase is an important allosteric enzyme in carbohydrate metabolism. Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known phosphorylases share catalytic and structural properties.

Evolutionary Conservation

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

See Also

2gm9, resolution 2.30Å

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