2v0g
From Proteopedia
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|PDB= 2v0g |SIZE=350|CAPTION= <scene name='initialview01'>2v0g</scene>, resolution 3.50Å | |PDB= 2v0g |SIZE=350|CAPTION= <scene name='initialview01'>2v0g</scene>, resolution 3.50Å | ||
|SITE= <scene name='pdbsite=AC1:LEU+Binding+Site+For+Chain+D'>AC1</scene> | |SITE= <scene name='pdbsite=AC1:LEU+Binding+Site+For+Chain+D'>AC1</scene> | ||
| - | |LIGAND= <scene name='pdbligand= | + | |LIGAND= <scene name='pdbligand=A:ADENOSINE-5'-MONOPHOSPHATE'>A</scene>, <scene name='pdbligand=ANZ:[(6-AMINO-9H-PURIN-9-YL)-[5-FLUORO-1,3-DIHYDRO-1-HYDROXY-2,1-BENZOXABOROLE]-4'YL]METHYL+DIHYDROGEN+PHOSPHATE'>ANZ</scene>, <scene name='pdbligand=C:CYTIDINE-5'-MONOPHOSPHATE'>C</scene>, <scene name='pdbligand=G:GUANOSINE-5'-MONOPHOSPHATE'>G</scene>, <scene name='pdbligand=HG:MERCURY+(II)+ION'>HG</scene>, <scene name='pdbligand=LEU:LEUCINE'>LEU</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=U:URIDINE-5'-MONOPHOSPHATE'>U</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2v0g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2v0g OCA], [http://www.ebi.ac.uk/pdbsum/2v0g PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2v0g RCSB]</span> | ||
}} | }} | ||
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[[Category: Zhang, Y.]] | [[Category: Zhang, Y.]] | ||
[[Category: Zhou, H.]] | [[Category: Zhou, H.]] | ||
| - | [[Category: HG]] | ||
| - | [[Category: LEU]] | ||
| - | [[Category: SO4]] | ||
| - | [[Category: ZN]] | ||
[[Category: aminoacyl-trna synthetase]] | [[Category: aminoacyl-trna synthetase]] | ||
[[Category: atp + l-leucine + trna (leu) gives amp + ppi l-leucyl-trna synthetase]] | [[Category: atp + l-leucine + trna (leu) gives amp + ppi l-leucyl-trna synthetase]] | ||
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[[Category: synthetase]] | [[Category: synthetase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:07:00 2008'' |
Revision as of 02:07, 31 March 2008
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| , resolution 3.50Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | |||||||
| Ligands: | , , , , , , , , | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
LEUCYL-TRNA SYNTHETASE FROM THERMUS THERMOPHILUS COMPLEXED WITH A TRNA(LEU) TRANSCRIPT WITH 5-FLUORO-1,3-DIHYDRO-1-HYDROXY-2,1-BENZOXABOROLE (AN2690) FORMING AN ADDUCT TO THE RIBOSE OF ADENOSINE-76 IN THE ENZYME EDITING SITE.
Overview
Aminoacyl-transfer RNA (tRNA) synthetases, which catalyze the attachment of the correct amino acid to its corresponding tRNA during translation of the genetic code, are proven antimicrobial drug targets. We show that the broad-spectrum antifungal 5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), in development for the treatment of onychomycosis, inhibits yeast cytoplasmic leucyl-tRNA synthetase by formation of a stable tRNA(Leu)-AN2690 adduct in the editing site of the enzyme. Adduct formation is mediated through the boron atom of AN2690 and the 2'- and 3'-oxygen atoms of tRNA's3'-terminal adenosine. The trapping of enzyme-bound tRNA(Leu) in the editing site prevents catalytic turnover, thus inhibiting synthesis of leucyl-tRNA(Leu) and consequentially blocking protein synthesis. This result establishes the editing site as a bona fide target for aminoacyl-tRNA synthetase inhibitors.
About this Structure
2V0G is a Protein complex structure of sequences from Thermus thermophilus. Full crystallographic information is available from OCA.
Reference
An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site., Rock FL, Mao W, Yaremchuk A, Tukalo M, Crepin T, Zhou H, Zhang YK, Hernandez V, Akama T, Baker SJ, Plattner JJ, Shapiro L, Martinis SA, Benkovic SJ, Cusack S, Alley MR, Science. 2007 Jun 22;316(5832):1759-61. PMID:17588934
Page seeded by OCA on Mon Mar 31 05:07:00 2008
Categories: Protein complex | Thermus thermophilus | Akama, T. | Alley, M R.K. | Baker, S. | Benkovic, S J. | Crepin, T. | Cusack, S. | Hernandez, V. | Mao, W. | Martinis, S A. | Plattner, J. | Rock, F. | Shapiro, L. | Tukalo, M. | Yaremchuk, A. | Zhang, Y. | Zhou, H. | Aminoacyl-trna synthetase | Atp + l-leucine + trna (leu) gives amp + ppi l-leucyl-trna synthetase | Atp- binding | Class i aminoacyl- trna synthetase | Editing | Ligase | Metal-binding | Nucleotide-binding zinc | Protein biosynthesis | Synthetase
