7q1b: Difference between revisions

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'''Unreleased structure'''


The entry 7q1b is ON HOLD
==Crystal structure of Trypanosoma cruzi histone deacetylase DAC2 complexed with Quisinostat==
<StructureSection load='7q1b' size='340' side='right'caption='[[7q1b]], [[Resolution|resolution]] 1.75&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[7q1b]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Trypanosoma_cruzi Trypanosoma cruzi]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7Q1B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7Q1B 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]] 1.75&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GOK:2-[4-[[(1-methylindol-3-yl)methylamino]methyl]piperidin-1-yl]-~{N}-oxidanyl-pyrimidine-5-carboxamide'>GOK</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</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=7q1b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7q1b OCA], [https://pdbe.org/7q1b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7q1b RCSB], [https://www.ebi.ac.uk/pdbsum/7q1b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7q1b ProSAT]</span></td></tr>
</table>
== Function ==
[https://www.uniprot.org/uniprot/A0A1B1JH81_TRYCR A0A1B1JH81_TRYCR]
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Writing and erasing of posttranslational modifications are crucial to phenotypic plasticity and antigenic variation of eukaryotic pathogens. Targeting pathogens' modification machineries, thus, represents a valid approach to fighting parasitic diseases. However, identification of parasitic targets and the development of selective anti-parasitic drugs still represent major bottlenecks. Here, we show that the zinc-dependent histone deacetylases (HDACs) of the protozoan parasite Trypanosoma cruzi are key regulators that have significantly diverged from their human counterparts. Depletion of T. cruzi class I HDACs tcDAC1 and tcDAC2 compromises cell-cycle progression and division, leading to cell death. Notably, tcDAC2 displays a deacetylase activity essential to the parasite and shows major structural differences with human HDACs. Specifically, tcDAC2 harbors a modular active site with a unique subpocket targeted by inhibitors showing substantial anti-parasitic effects in cellulo and in vivo. Thus, the targeting of the many atypical HDACs in pathogens can enable anti-parasitic selective chemical impairment.


Authors: Marek, M., Ramos-Morales, E., Romier, C.
Species-selective targeting of pathogens revealed by the atypical structure and active site of Trypanosoma cruzi histone deacetylase DAC2.,Marek M, Ramos-Morales E, Picchi-Constante GFA, Bayer T, Norstrom C, Herp D, Sales-Junior PA, Guerra-Slompo EP, Hausmann K, Chakrabarti A, Shaik TB, Merz A, Troesch E, Schmidtkunz K, Goldenberg S, Pierce RJ, Mourao MM, Jung M, Schultz J, Sippl W, Zanchin NIT, Romier C Cell Rep. 2021 Dec 21;37(12):110129. doi: 10.1016/j.celrep.2021.110129. PMID:34936867<ref>PMID:34936867</ref>


Description: Crystal structure of Trypanosoma cruzi histone deacetylase DAC2 complexed with Quisinostat
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
[[Category: Unreleased Structures]]
</div>
[[Category: Romier, C]]
<div class="pdbe-citations 7q1b" style="background-color:#fffaf0;"></div>
[[Category: Ramos-Morales, E]]
 
[[Category: Marek, M]]
==See Also==
*[[Histone deacetylase 3D structures|Histone deacetylase 3D structures]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Large Structures]]
[[Category: Trypanosoma cruzi]]
[[Category: Marek M]]
[[Category: Ramos-Morales E]]
[[Category: Romier C]]
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