1zz1: Difference between revisions

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New page: left|200px<br /><applet load="1zz1" size="450" color="white" frame="true" align="right" spinBox="true" caption="1zz1, resolution 1.57Å" /> '''Crystal structure of...
 
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[[Image:1zz1.gif|left|200px]]<br /><applet load="1zz1" size="450" color="white" frame="true" align="right" spinBox="true"
caption="1zz1, resolution 1.57&Aring;" />
'''Crystal structure of a HDAC-like protein with SAHA bound'''<br />


==Overview==
==Crystal structure of a HDAC-like protein with SAHA bound==
Histone deacetylases (HDACs) are among the most promising targets in, cancer therapy. However, structural information greatly enhancing the, design of HDAC inhibitors as novel chemotherapeutics has not been, available on class 2 HDACs so far. Here we present the structure of the, bacterial FB188 HDAH (histone deacetylase-like amidohydrolase from, Bordetella/Alcaligenes strain FB188) that reveals high sequential and, functional homology to human class 2 HDACs. FB188 HDAH is capable to, remove the acetyl moiety from acetylated histones. Several HDAC-specific, inhibitors, which have been shown to inhibit tumor activity in both, pre-clinical models and in clinical trials, also inhibit FB188 HDAH. We, have determined the crystal structure of FB188 HDAH at a resolution of 1.6, angstroms in complex with the reaction product acetate, as well as in, complex with the inhibitors suberoylanilide hydroxamic acid (SAHA) and, cyclopentyle-propionyle hydroxamic acid (CypX) at a resolution of 1.57, angstroms and 1.75 angstroms, respectively. FB188 HDAH exhibits the, canonical fold of class 1 HDACs and contains a catalytic zinc ion. The, highest structural diversity compared to class 1 enzymes is found in loop, regions especially in the area around the entrance of the active site, indicating significant differences among the acetylated proteins binding, to class 1 and 2 HDACs, respectively.
<StructureSection load='1zz1' size='340' side='right'caption='[[1zz1]], [[Resolution|resolution]] 1.57&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[1zz1]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Alcaligenaceae_bacterium_FB188 Alcaligenaceae bacterium FB188]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1ZZ1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1ZZ1 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]] 1.57&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=K:POTASSIUM+ION'>K</scene>, <scene name='pdbligand=SHH:OCTANEDIOIC+ACID+HYDROXYAMIDE+PHENYLAMIDE'>SHH</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=1zz1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1zz1 OCA], [https://pdbe.org/1zz1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1zz1 RCSB], [https://www.ebi.ac.uk/pdbsum/1zz1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1zz1 ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/HDAH_ALCSD HDAH_ALCSD]
== 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/zz/1zz1_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=1zz1 ConSurf].
<div style="clear:both"></div>


==About this Structure==
==See Also==
1ZZ1 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Bordetella_sp. Bordetella sp.] with ZN, K and SHH as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1ZZ1 OCA].
*[[Histone deacetylase 3D structures|Histone deacetylase 3D structures]]
 
__TOC__
==Reference==
</StructureSection>
Crystal structure of a bacterial class 2 histone deacetylase homologue., Nielsen TK, Hildmann C, Dickmanns A, Schwienhorst A, Ficner R, J Mol Biol. 2005 Nov 18;354(1):107-20. Epub 2005 Oct 7. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16242151 16242151]
[[Category: Alcaligenaceae bacterium FB188]]
[[Category: Bordetella sp.]]
[[Category: Large Structures]]
[[Category: Single protein]]
[[Category: Dickmanns A]]
[[Category: Dickmanns, A.]]
[[Category: Ficner R]]
[[Category: Ficner, R.]]
[[Category: Hildmann C]]
[[Category: Hildmann, C.]]
[[Category: Nielsen TK]]
[[Category: Nielsen, T.K.]]
[[Category: Schwienhorst A]]
[[Category: Schwienhorst, A.]]
[[Category: K]]
[[Category: SHH]]
[[Category: ZN]]
[[Category: hydrolase]]
 
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Wed Nov 21 07:45:10 2007''

Latest revision as of 16:39, 13 March 2024

Crystal structure of a HDAC-like protein with SAHA boundCrystal structure of a HDAC-like protein with SAHA bound

Structural highlights

1zz1 is a 4 chain structure with sequence from Alcaligenaceae bacterium FB188. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.57Å
Ligands:, ,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

HDAH_ALCSD

Evolutionary Conservation

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

See Also

1zz1, resolution 1.57Å

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