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3q2m

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Crystal Structure of Spectinomycin Phosphotransferase, APH(9)-Ia, Protein Kinase Inhibitor CKI-7 Complex

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Retrieved from "http://52.214.119.220/wiki/index.php/3q2m"

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 == Structural highlights ==
 <table><tr><td colspan='2'>[[3q2m]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Legionella_pneumophila_130b Legionella pneumophila 130b]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3Q2M OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3Q2M FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CKI:N-(2-AMINOETHYL)-5-CHLOROISOQUINOLINE-8-SULFONAMIDE'>CKI</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.9&#8491;</td></tr>
-<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3i0o|3i0o]], [[3i0q|3i0q]], [[3i1a|3i1a]]</div></td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CKI:N-(2-AMINOETHYL)-5-CHLOROISOQUINOLINE-8-SULFONAMIDE'>CKI</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene></td></tr>
-<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">aph, LPW_21961 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=866628 Legionella pneumophila 130b])</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=3q2m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3q2m OCA], [https://pdbe.org/3q2m PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3q2m RCSB], [https://www.ebi.ac.uk/pdbsum/3q2m PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3q2m ProSAT]</span></td></tr>
 </table>
-<div style="background-color:#fffaf0;">
+== Function ==
-== Publication Abstract from PubMed ==
+[https://www.uniprot.org/uniprot/O06916_LEGPN O06916_LEGPN]
-Antibiotic resistance is recognized as a growing healthcare problem. To address this issue, one strategy is to thwart the causal mechanism using an adjuvant in partner with the antibiotic. Aminoglycosides are a class of clinically important antibiotics used for the treatment of serious infections. Their usefulness has been compromised predominantly due to drug inactivation by aminoglycoside-modifying enzymes, such as aminoglycoside phosphotransferases or kinases. These kinases are structurally homologous to eukaryotic Ser/Thr and Tyr protein kinases and it has been shown that some can be inhibited by select protein kinase inhibitors. The aminoglycoside kinase, APH(3')-IIIa, can be inhibited by CKI-7, an ATP-competitive inhibitor for the casein kinase 1. We have determined that CKI-7 is also a moderate inhibitor for the atypical APH(9)-Ia. Here we present the crystal structures of CKI-7-bound APH(3')-IIIa and APH(9)-Ia, the first structures of a eukaryotic protein kinase inhibitor in complex with bacterial kinases. CKI-7 binds to the nucleotide-binding pocket of the enzymes and its binding alters the conformation of the nucleotide-binding loop, the segment homologous to the glycine-rich loop in eukaryotic protein kinases. Comparison of these structures with the CKI-7-bound casein kinase 1 reveals features in the binding pockets that are distinct in the bacterial kinases and could be exploited for the design of a bacterial kinase specific inhibitor. Our results provide evidence that an inhibitor for a subset of APHs can be developed in order to curtail resistance to aminoglycosides.
-Crystal structures of two aminoglycoside kinases bound with a eukaryotic protein kinase inhibitor.,Fong DH, Xiong B, Hwang J, Berghuis AM PLoS One. 2011 May 9;6(5):e19589. doi: 10.1371/journal.pone.0019589. PMID:21573013<ref>PMID:21573013</ref>
-From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-</div>
-<div class="pdbe-citations 3q2m" style="background-color:#fffaf0;"></div>
 ==See Also==
 *[[Phosphotransferase 3D structures|Phosphotransferase 3D structures]]
-== References ==
-<references/>
 __TOC__
 </StructureSection>
 [[Category: Large Structures]]
 [[Category: Legionella pneumophila 130b]]
-[[Category: Berghuis, A M]]
+[[Category: Berghuis AM]]
-[[Category: Fong, D H]]
+[[Category: Fong DH]]
-[[Category: Hwang, J]]
+[[Category: Hwang J]]
-[[Category: Xiong, B]]
+[[Category: Xiong B]]
-[[Category: Cytosol]]
-[[Category: Phosphorylation]]
-[[Category: Phosphotransferase]]
-[[Category: Ser/thr/tyr protein kinase]]
-[[Category: Transferase-transferase inhibitor complex]]

3q2m

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Crystal Structure of Spectinomycin Phosphotransferase, APH(9)-Ia, Protein Kinase Inhibitor CKI-7 Complex

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