Top ▲

DNA gyrase

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 3219

Nomenclature: DNA gyrase

Family: Bacterial protein targets

Quaternary Structure: Subunits
DNA gyrase subunit A
DNA gyrase subunit B
Quaternary Structure Comments
DNA gyrase is a tetrameric enzyme, consisting of DNA gyrase A and B subunits assembled into a A2B2 complex of approximatively 370 kDa [3].
Database Links Click here for help
ChEMBL Target

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BWC0977 Small molecule or natural product Click here for species-specific activity table E.coli Inhibition 8.4 pIC50
pIC50 8.4 (IC50 4x10-9 M)
zoliflodacin Small molecule or natural product Ligand has a PDB structure E.coli - 6.8 pIC50 1
pIC50 6.8 (IC50 1.69x10-7 M) [1]
Description: DNA gyrase supercoiling assay
General Comments
DNA gyrase is a type II DNA topoisomerase [2] and one of two enzymes of this subclass found in bacteria, the other being DNA topoisomerase 4. DNA gyrase introduces negative supercoils in closed circular double-stranded DNA in an ATP-dependent manner.
This enzyme is the clinically-validated target for a number of antibacterial drug classes, including the aminocoumarins and fluoroquinolones.

References

Show »

1. Basarab GS, Gowravaram MR, Hauck SI, Zhou F. (2014) Compounds and methods for treating bacterial infections. Patent number: US8889671B2. Assignee: Entasis Therapeutics. Priority date: 23/01/2013. Publication date: 18/11/2014.

2. Gellert M, Mizuuchi K, O'Dea MH, Nash HA. (1976) DNA gyrase: an enzyme that introduces superhelical turns into DNA. Proc Natl Acad Sci U S A, 73 (11): 3872-6. [PMID:186775]

3. Vanden Broeck A, Lotz C, Ortiz J, Lamour V. (2019) Cryo-EM structure of the complete E. coli DNA gyrase nucleoprotein complex. Nat Commun, 10 (1): 4935. [PMID:31666516]

How to cite this page

Bacterial protein targets: DNA gyrase. Last modified on 04/08/2023. Accessed on 08/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3219.