ArticleNature chemistry2020
Repurposing human kinase inhibitors to create an antibiotic active against drug-resistant Staphylococcus aureus, persisters and biofilms.
Article in Nature chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 67 papers.
What it found
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Who cites it
67 citing papers in PubMed, 138 citations in OpenAlex.
- Targeting a Myeloid-Regulatory B Cell Network Reverses Immune Paralysis in Periprosthetic Joint Infections.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Dual host and pathogen targeting by MEK1/2 inhibitors.Infection and immunity · 2026Review
- Article
- Host-Pathogen Dual Targeting With Repurposed Drugs Identifies a Synergistic Therapy for Intracellular Staphylococcus aureus.MicrobiologyOpen · 2026Article
- Tunable TriPcides suppress virulence factor secretion duringScience advances · 2026Article
- Proteomic approaches for interrogating kinase signaling networks.The Journal of investigative dermatology · 2026Article
- Fighting the invader: strategies against intracellular bacteria.Frontiers in pharmacology · 2026Review
- Multifaceted Small Molecules as Enzyme Modulators: Cases of Drug Discovery/Repurposing Illustrating Nature's Pragmatism.BioMed research international · 2026Review
- Lapatinib-Loaded ZIF‑8 Nanoparticles: A Multifunctional Drug Delivery System with Anticancer, Antibacterial, and Antioxidant Properties.ACS omega · 2025Article
- Structural and evolutionary insights into understudied bacterial serine-threonine pseudokinase families.Biochemical Society transactions · 2025Review
- Drug Repurposing: An Emerging Strategy inJournal of microbiology and biotechnology · 2025Review
- Repurposing a drug to punish carbapenem-resistantProceedings of the National Academy of Sciences of the United States of America · 2025Article
- Tailored phenyl ureas eradicate drug-resistantChemical science · 2025Article
- Antibacterial compounds against non-growing and intracellular bacteria.npj antimicrobials and resistance · 2025Article
- Chemoproteomic Profiling ofJournal of medicinal chemistry · 2025Article
- From Natural Products to Small Molecules: Recent Advancements in Anti-MRSA Therapeutics.ACS medicinal chemistry letters · 2025Review
- Non-Membrane Active Peptide Resensitizes MRSA to β-Lactam Antibiotics and Inhibits S. aureus Virulence.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Synthetic Cation Transporters Eradicate Drug-ResistantJACS Au · 2025Article
- Antibiotic target discovery by integrated phenotypic and activity-based profiling of electrophilic fragments.Cell chemical biology · 2025Article
- Fighting Antimicrobial Resistance: Innovative Drugs in Antibacterial Research.Angewandte Chemie (International ed. in English) · 2025Review
7 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
21 authors at 7 institutions in 3 countries.
Funding
Abstract
New drugs are desperately needed to combat methicillin-resistant Staphylococcus aureus (MRSA) infections. Here, we report screening commercial kinase inhibitors for antibacterial activity and found the anticancer drug sorafenib as major hit that effectively kills MRSA strains. Varying the key structural features led to the identification of a potent analogue, PK150, that showed antibacterial activity against several pathogenic strains at submicromolar concentrations. Furthermore, this antibiotic eliminated challenging persisters as well as established biofilms. PK150 holds promising therapeutic potential as it did not induce in vitro resistance, and shows oral bioavailability and in vivo efficacy. Analysis of the mode of action using chemical proteomics revealed several targets, which included interference with menaquinone biosynthesis by inhibiting demethylmenaquinone methyltransferase and the stimulation of protein secretion by altering the activity of signal peptidase IB. Reduced endogenous menaquinone levels along with enhanced levels of extracellular proteins of PK150-treated bacteria support this target hypothesis. The associated antibiotic effects, especially the lack of resistance development, probably stem from the compound's polypharmacology.
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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.