1jik: Difference between revisions

Revision as of 14:23, 21 February 2008

Crystal structure of S. aureus TyrRS in complex with SB-243545

OverviewOverview

SB-219383 and its analogues are a class of potent and specific inhibitors of bacterial tyrosyl-tRNA synthetases. Crystal structures of these inhibitors have been solved in complex with the tyrosyl-tRNA synthetase from Staphylococcus aureus, the bacterium that is largely responsible for hospital-acquired infections. The full-length enzyme yielded crystals that diffracted to 2.8 A resolution, but a truncated version of the enzyme allowed the resolution to be extended to 2.2 A. These inhibitors not only occupy the known substrate binding sites in unique ways, but also reveal a butyl binding pocket. It was reported that the Bacillus stearothermophilus TyrRS T51P mutant has much increased catalytic activity. The S. aureus enzyme happens to have a proline at position 51. Therefore, our structures may contribute to the understanding of the catalytic mechanism and provide the structural basis for designing novel antimicrobial agents.

About this StructureAbout this Structure

1JIK is a Single protein structure of sequence from Staphylococcus aureus with as ligand. Active as Tyrosine--tRNA ligase, with EC number 6.1.1.1 Full crystallographic information is available from OCA.

ReferenceReference

Crystal structure of Staphylococcus aureus tyrosyl-tRNA synthetase in complex with a class of potent and specific inhibitors., Qiu X, Janson CA, Smith WW, Green SM, McDevitt P, Johanson K, Carter P, Hibbs M, Lewis C, Chalker A, Fosberry A, Lalonde J, Berge J, Brown P, Houge-Frydrych CS, Jarvest RL, Protein Sci. 2001 Oct;10(10):2008-16. PMID:11567092

Page seeded by OCA on Thu Feb 21 13:23:04 2008

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OCA

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-[[Image:1jik.jpg|left|200px]]<br /><applet load="1jik" size="450" color="white" frame="true" align="right" spinBox="true"
+[[Image:1jik.jpg|left|200px]]<br /><applet load="1jik" size="350" color="white" frame="true" align="right" spinBox="true"
 caption="1jik, resolution 2.80&Aring;" />
 '''Crystal structure of S. aureus TyrRS in complex with SB-243545'''<br />
 ==Overview==
-SB-219383 and its analogues are a class of potent and specific inhibitors, of bacterial tyrosyl-tRNA synthetases. Crystal structures of these, inhibitors have been solved in complex with the tyrosyl-tRNA synthetase, from Staphylococcus aureus, the bacterium that is largely responsible for, hospital-acquired infections. The full-length enzyme yielded crystals that, diffracted to 2.8 A resolution, but a truncated version of the enzyme, allowed the resolution to be extended to 2.2 A. These inhibitors not only, occupy the known substrate binding sites in unique ways, but also reveal a, butyl binding pocket. It was reported that the Bacillus stearothermophilus, TyrRS T51P mutant has much increased catalytic activity. The S. aureus, enzyme happens to have a proline at position 51. Therefore, our structures, may contribute to the understanding of the catalytic mechanism and provide, the structural basis for designing novel antimicrobial agents.
+SB-219383 and its analogues are a class of potent and specific inhibitors of bacterial tyrosyl-tRNA synthetases. Crystal structures of these inhibitors have been solved in complex with the tyrosyl-tRNA synthetase from Staphylococcus aureus, the bacterium that is largely responsible for hospital-acquired infections. The full-length enzyme yielded crystals that diffracted to 2.8 A resolution, but a truncated version of the enzyme allowed the resolution to be extended to 2.2 A. These inhibitors not only occupy the known substrate binding sites in unique ways, but also reveal a butyl binding pocket. It was reported that the Bacillus stearothermophilus TyrRS T51P mutant has much increased catalytic activity. The S. aureus enzyme happens to have a proline at position 51. Therefore, our structures may contribute to the understanding of the catalytic mechanism and provide the structural basis for designing novel antimicrobial agents.
 ==About this Structure==
-JIK is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus] with 545 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Tyrosine--tRNA_ligase Tyrosine--tRNA ligase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=6.1.1.1 6.1.1.1] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1JIK OCA].
+JIK is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Staphylococcus_aureus Staphylococcus aureus] with <scene name='pdbligand=545:'>545</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [http://en.wikipedia.org/wiki/Tyrosine--tRNA_ligase Tyrosine--tRNA ligase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=6.1.1.1 6.1.1.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1JIK OCA].
 ==Reference==
@@ Line 14: / Line 14: @@
 [[Category: Staphylococcus aureus]]
 [[Category: Tyrosine--tRNA ligase]]
-[[Category: Janson, C.A.]]
+[[Category: Janson, C A.]]
-[[Category: Jarvest, R.L.]]
+[[Category: Jarvest, R L.]]
 [[Category: Qiu, X.]]
-[[Category: Smith, W.W.]]
+[[Category: Smith, W W.]]
 [[Category: 545]]
 [[Category: staphylococcus aureus]]
@@ Line 24: / Line 24: @@
 [[Category: tyrosyl-trna synthetase]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Sat Nov 24 23:42:39 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:23:04 2008''