ArticleChemistry (Weinheim an der Bergstrasse, Germany)2022
Optical Modulation of Antibiotic Resistance by Photoswitchable Cystobactamids.
Article in Chemistry (Weinheim an der Bergstrasse, Germany), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 12 citations in OpenAlex.
- Effects of Supramolecular Interactions on E/Z-Isomerizations in Water and Their Importance for Biological Applications.Archiv der Pharmazie · 2026Review
- Synthesis, photochemical and biological evaluation of novel photoswitchable glycomimetic ligands ofRSC advances · 2025Article
- Synthesis of Tetra-The Journal of organic chemistry · 2024Article
- Light-Based Anti-Biofilm and Antibacterial Strategies.Pharmaceutics · 2023Review
- Exploring antibiotic resistance with chemical tools.Chemical communications (Cambridge, England) · 2023Review
- Transcription activation by the resistance protein AlbA as a tool to evaluate derivatives of the antibiotic albicidin.Chemical science · 2023Article
- Optical Modulation of Antibiotic Resistance by Photoswitchable Cystobactamids.Chemistry (Weinheim an der Bergstrasse, Germany) · 2022Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
The rise of antibiotic resistance causes a serious health care problem, and its counterfeit demands novel, innovative concepts. The combination of photopharmacology, enabling a light-controlled reversible modulation of drug activity, with antibiotic drug design has led to first photoswitchable antibiotic compounds derived from established scaffolds. In this study, we converted cystobactamids, gyrase-inhibiting natural products with an oligoaryl scaffold and highly potent antibacterial activities, into photoswitchable agents by inserting azobenzene in the N-terminal part and/or an acylhydrazone moiety near the C-terminus, yielding twenty analogs that contain mono- as well as double-switches. Antibiotic and gyrase inhibition properties could be modulated 3.4-fold and 5-fold by light, respectively. Notably, the sensitivity of photoswitchable cystobactamids towards two known resistance factors, the peptidase AlbD and the scavenger protein AlbA, was light-dependent. While irradiation of an analog with an N-terminal azobenzene with 365 nm light led to less degradation by AlbD, the AlbA-mediated inactivation was induced. This provides a proof-of-principle that resistance towards photoswitchable antibiotics can be optically controlled.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.