ArticleChemical biology & drug design2020
Eukaryotic phosphatase inhibitors enhance colistin efficacy in gram-negative bacteria.
Article in Chemical biology & drug design, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 9 citations in OpenAlex.
- Therapeutic Potential of Kuwanon G: From Bioactivities to Network-Level Mechanisms.Molecules (Basel, Switzerland) · 2026Review
- Notoginsenoside Ft1 enhances the effectiveness of gentamicin against Escherichia coli by interfering with intrinsic antibacterial mechanisms.BMC microbiology · 2025Article
- Synergistic Activity and Mechanism of Sanguinarine with Polymyxin B against Gram-Negative Bacterial Infections.Pharmaceutics · 2024Article
- Famotidine Enhances Rifampicin Activity against Acinetobacter baumannii by Affecting OmpA.Journal of bacteriology · 2023Article
- Identification of potential RapJ hits as sporulation pathway inducer candidates in Bacillus coagulans via structure-based virtual screening and molecular dynamics simulation studies.Journal of molecular modeling · 2023Article
- Mulberry Diels-Alder-type adducts: isolation, structure, bioactivity, and synthesis.Natural products and bioprospecting · 2022Review
- Phenotypic screening of compound libraries as a platform for the identification of antibiotic adjuvants: Identification of colistin adjuvants from a natural product library.Methods in enzymology · 2022Article
- Benzimidazole Isosteres of Salicylanilides Are Highly Active Colistin Adjuvants.ACS infectious diseases · 2021Article
- How to Combat Gram-Negative Bacteria Using Antimicrobial Peptides: A Challenge or an Unattainable Goal?Antibiotics (Basel, Switzerland) · 2021Review
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
The mounting threat of multi-drug-resistant (MDR) bacteria places a tremendous strain on the antimicrobial clinical arsenal, forcing physicians to revert to near-obsolete antibiotics to treat otherwise intractable infections. Antibiotic adjuvant therapy has emerged as a viable alternative to the development of novel antimicrobial agents. This method uses combinations of an existing antibiotic and a non-antimicrobial small molecule, where the combination either breaks drug resistance or further potentiates antibiotic activity. Through a high-content screen of eukaryotic kinase inhibitors, our group previously identified two highly potent adjuvants that synergize with colistin, a cyclic, polycationic antimicrobial peptide that serves as a drug of last resort for the treatment of MDR Gram-negative bacterial infections. Cell signaling proteins implicated in colistin resistance mechanisms display both kinase and phosphatase activities. Herein, we explore the potential for eukaryotic phosphatase inhibitors to be repurposed as colistin adjuvants. From a panel of 48 unique structures, we discovered that the natural product kuwanon G breaks colistin resistance, while the non-antimicrobial macrolide ascomycin potentiates colistin in polymyxin-susceptible bacteria.
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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.