Molecular mechanism of topoisomerase poisoning by the peptide antibiotic albicidin.
Antibiotics
Enzyme mechanisms
Mechanism of action
Structure-based drug design
Target validation
Journal
Nature catalysis
ISSN: 2520-1158
Titre abrégé: Nat Catal
Pays: England
ID NLM: 101714581
Informations de publication
Date de publication:
2023
2023
Historique:
received:
02
06
2022
accepted:
30
11
2022
entrez:
6
2
2023
pubmed:
7
2
2023
medline:
7
2
2023
Statut:
ppublish
Résumé
The peptide antibiotic albicidin is a DNA topoisomerase inhibitor with low-nanomolar bactericidal activity towards fluoroquinolone-resistant Gram-negative pathogens. However, its mode of action is poorly understood. We determined a 2.6 Å resolution cryoelectron microscopy structure of a ternary complex between
Identifiants
pubmed: 36741192
doi: 10.1038/s41929-022-00904-1
pii: 904
pmc: PMC9886550
doi:
Types de publication
Journal Article
Langues
eng
Pagination
52-67Subventions
Organisme : Biotechnology and Biological Sciences Research Council
ID : BBS/E/J/000PR9790
Pays : United Kingdom
Informations de copyright
© The Author(s) 2023.
Déclaration de conflit d'intérêts
Competing interestsThe following authors declare competing interests. R.D.S. is inventor of patent EP2956437A1. R.D.S., I.B. and J.W. are inventors of patents EP3655394A1 and EP3655394A1. R.D.S., K.H., I.B. and J.W. are inventors of patent EP3974416A1. R.D.S., M.K., K.H., L.Z. and J.W. are inventors of patent EP22163715.0. All listed patents have been filed at the TU Berlin and are describing the synthesis and use of albicidin and derivatives thereof. Synthesis of albicidin derivatives published in the manuscript NATCATAL-22067343A are covered by the aforementioned patents. R.D.S. is a consultant to Selmod GmbH. The remaining authors have no conflicts of interest to declare.
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