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==Crystal Structure of Spectinomycin Phosphotransferase, APH(9)-Ia, Protein Kinase Inhibitor CKI-7 Complex==
==Crystal Structure of Spectinomycin Phosphotransferase, APH(9)-Ia, Protein Kinase Inhibitor CKI-7 Complex==
<StructureSection load='3q2m' size='340' side='right' caption='[[3q2m]], [[Resolution|resolution]] 2.90&Aring;' scene=''>
<StructureSection load='3q2m' size='340' side='right'caption='[[3q2m]], [[Resolution|resolution]] 2.90&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[3q2m]] is a 1 chain structure with sequence from [http://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 [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3Q2M FirstGlance]. <br>
<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"><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">[[3i0o|3i0o]], [[3i0q|3i0q]], [[3i1a|3i1a]]</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 ([http://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>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3q2m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3q2m OCA], [http://pdbe.org/3q2m PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3q2m RCSB], [http://www.ebi.ac.uk/pdbsum/3q2m PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3q2m ProSAT]</span></td></tr>
</table>
</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==
==See Also==
*[[Phosphotransferase|Phosphotransferase]]
*[[Phosphotransferase 3D structures|Phosphotransferase 3D structures]]
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Large Structures]]
[[Category: Legionella pneumophila 130b]]
[[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]]

Latest revision as of 14:30, 14 March 2024

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

Structural highlights

3q2m is a 1 chain structure with sequence from Legionella pneumophila 130b. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 2.9Å
Ligands:,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

O06916_LEGPN

See Also

3q2m, resolution 2.90Å

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