3r1k

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Current revision (10:51, 21 February 2024) (edit) (undo)
 
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<StructureSection load='3r1k' size='340' side='right'caption='[[3r1k]], [[Resolution|resolution]] 1.95&Aring;' scene=''>
<StructureSection load='3r1k' size='340' side='right'caption='[[3r1k]], [[Resolution|resolution]] 1.95&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[3r1k]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/"bacillus_tuberculosis"_(zopf_1883)_klein_1884 "bacillus tuberculosis" (zopf 1883) klein 1884]. The February 2012 RCSB PDB [https://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/index.html Molecule of the Month] feature on ''Aminoglycoside Antibiotics'' by David Goodsell is [https://dx.doi.org/10.2210/rcsb_pdb/mom_2012_2 10.2210/rcsb_pdb/mom_2012_2]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3R1K OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3R1K FirstGlance]. <br>
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<table><tr><td colspan='2'>[[3r1k]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Mycobacterium_tuberculosis Mycobacterium tuberculosis]. The February 2012 RCSB PDB [https://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/index.html Molecule of the Month] feature on ''Aminoglycoside Antibiotics'' by David Goodsell is [https://dx.doi.org/10.2210/rcsb_pdb/mom_2012_2 10.2210/rcsb_pdb/mom_2012_2]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3R1K OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3R1K FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACM:ACETAMIDE'>ACM</scene>, <scene name='pdbligand=COA:COENZYME+A'>COA</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.95&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">eis, Rv2416c, MT2489, MTCY253.04 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=1773 "Bacillus tuberculosis" (Zopf 1883) Klein 1884])</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACM:ACETAMIDE'>ACM</scene>, <scene name='pdbligand=COA:COENZYME+A'>COA</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=3r1k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3r1k OCA], [https://pdbe.org/3r1k PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3r1k RCSB], [https://www.ebi.ac.uk/pdbsum/3r1k PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3r1k ProSAT]</span></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=3r1k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3r1k OCA], [https://pdbe.org/3r1k PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3r1k RCSB], [https://www.ebi.ac.uk/pdbsum/3r1k PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3r1k ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[https://www.uniprot.org/uniprot/EIS_MYCTU EIS_MYCTU]] May participate in pathogenesis, possibly by enhancing survival of the bacteria in host macrophages during infection.<ref>PMID:10629183</ref>
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[https://www.uniprot.org/uniprot/EIS_MYCTU EIS_MYCTU] May participate in pathogenesis, possibly by enhancing survival of the bacteria in host macrophages during infection.<ref>PMID:10629183</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The emergence of multidrug-resistant and extensively drug-resistant (XDR) tuberculosis (TB) is a serious global threat. Aminoglycoside antibiotics are used as a last resort to treat XDR-TB. Resistance to the aminoglycoside kanamycin is a hallmark of XDR-TB. Here, we reveal the function and structure of the mycobacterial protein Eis responsible for resistance to kanamycin in a significant fraction of kanamycin-resistant Mycobacterium tuberculosis clinical isolates. We demonstrate that Eis has an unprecedented ability to acetylate multiple amines of many aminoglycosides. Structural and mutagenesis studies of Eis indicate that its acetylation mechanism is enabled by a complex tripartite fold that includes two general control non-derepressible 5 (GCN5)-related N-acetyltransferase regions. An intricate negatively charged substrate-binding pocket of Eis is a potential target of new antitubercular drugs expected to overcome aminoglycoside resistance.
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Unusual regioversatility of acetyltransferase Eis, a cause of drug resistance in XDR-TB.,Chen W, Biswas T, Porter VR, Tsodikov OV, Garneau-Tsodikova S Proc Natl Acad Sci U S A. 2011 May 31. PMID:21628583<ref>PMID:21628583</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 3r1k" style="background-color:#fffaf0;"></div>
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== References ==
== References ==
<references/>
<references/>
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[[Category: Aminoglycoside Antibiotics]]
[[Category: Aminoglycoside Antibiotics]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Mycobacterium tuberculosis]]
[[Category: RCSB PDB Molecule of the Month]]
[[Category: RCSB PDB Molecule of the Month]]
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[[Category: Biswas, T]]
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[[Category: Biswas T]]
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[[Category: Chen, W]]
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[[Category: Chen W]]
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[[Category: Garneau-Tsodikova, S]]
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[[Category: Garneau-Tsodikova S]]
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[[Category: Tsodikov, O V]]
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[[Category: Tsodikov OV]]
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[[Category: Acetyltransferase]]
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[[Category: Gnat]]
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[[Category: Transferase]]
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Current revision

Crystal structure of acetyltransferase Eis from Mycobacterium tuberculosis H37Rv in complex with CoA and an acetamide moiety

PDB ID 3r1k

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