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DNA gyrase subunit A

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Target not currently curated in GtoImmuPdb

Target id: 3217

Nomenclature: DNA gyrase subunit A

Family: Bacterial protein targets

Quaternary Structure: Complexes
DNA gyrase
Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Escherichia coli - 875 gyrA DNA gyrase subunit A
Database Links Click here for help
Alphafold
ChEMBL Target
Entrez Gene
RefSeq Protein
UniProtKB
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  59KDA fragment of gyrase A from E.coli
PDB Id:  1ab4
Resolution:  2.8Å
Species:  Escherichia coli
References:  3

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
LEI-800 Small molecule or natural product Ligand has a PDB structure E.coli - 7.5 pIC50 1
pIC50 7.5 (IC50 3.5x10-8 M) [1]
Description: DNA-supercoiling assay
ofloxacin Small molecule or natural product Approved drug E.coli - 5.5 pIC50 2
pIC50 5.5 (IC50 3.5x10-6 M) [2]
Description: DNA-supercoiling assay
General Comments
DNA gyrase subunit A is comprised of an N-terminal domain (59-64 kDa) involved in DNA cleavage and ligation, and a C-terminal domain (33 kDa) involved in DNA-protein interactions [4].

References

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1. Bakker AT, Kotsogianni I, Avalos M, Punt JM, Liu B, Piermarini D, Gagestein B, Slingerland CJ, Zhang L, Willemse JJ et al.. (2024) Discovery of isoquinoline sulfonamides as allosteric gyrase inhibitors with activity against fluoroquinolone-resistant bacteria. Nat Chem, 16 (9): 1462-1472. [PMID:38898213]

2. Barnard FM, Maxwell A. (2001) Interaction between DNA gyrase and quinolones: effects of alanine mutations at GyrA subunit residues Ser(83) and Asp(87). Antimicrob Agents Chemother, 45 (7): 1994-2000. [PMID:11408214]

3. Morais Cabral JH, Jackson AP, Smith CV, Shikotra N, Maxwell A, Liddington RC. (1997) Crystal structure of the breakage-reunion domain of DNA gyrase. Nature, 388 (6645): 903-6. [PMID:9278055]

4. Reece RJ, Maxwell A. (1989) Tryptic fragments of the Escherichia coli DNA gyrase A protein. J Biol Chem, 264 (33): 19648-53. [PMID:2555327]

How to cite this page

Bacterial protein targets: DNA gyrase subunit A. Last modified on 02/10/2024. Accessed on 08/02/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3217.