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DNA gyrase

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Target not currently curated in GtoImmuPdb

Target id: 3219

Nomenclature: DNA gyrase

Family: Bacterial protein targets

Contents:

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].
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ChEMBL Target CHEMBL2094139 (E.coli)

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Inhibitors
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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

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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 27/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=3219.