ArticleJournal of medicinal chemistry2023
Conjugation of Vancomycin with a Single Arginine Improves Efficacy against Mycobacteria by More Effective Peptidoglycan Targeting.
Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 18 citations in OpenAlex.
- A Siderophore-Antibiotic Heterodimer Imaging Agent EnablesJournal of medicinal chemistry · 2026Article
- Antibiotic hybrids: A promising strategy to replenish the pipeline and combat antimicrobial resistance.Journal of microbiology (Seoul, Korea) · 2026Review
- Vancomycin resistance in gram-positive infections: evolutionary strategies of survival.Archives of microbiology · 2026Review
- Guanidiniocarbonyl-Pyrrole (GCP) C- and N-Terminus Modifications of Vancomycin.The Journal of organic chemistry · 2025Article
- Vancomycin-Teixobactin Conjugates.Journal of the American Chemical Society · 2025Article
- New Conjugates of Vancomycin with Cell-Penetrating Peptides-Synthesis, Antimicrobial Activity, Cytotoxicity, and BBB Permeability Studies.Molecules (Basel, Switzerland) · 2024Article
- Tetrachloromaxamycins: Divergent Total Synthesis and Initial Assessments.The Journal of organic chemistry · 2024Article
- Biguanide-Vancomycin Conjugates are Effective Broad-Spectrum Antibiotics against Actively Growing and Biofilm-Associated Gram-Positive and Gram-Negative ESKAPE Pathogens and Mycobacteria.Journal of the American Chemical Society · 2024Article
- Synthesis and preclinical evaluation of novelEuropean journal of nuclear medicine and molecular imaging · 2024Article
- Antibiotic resistance inJAC-antimicrobial resistance · 2024Article
- Engineered Vancomycin, with Increased Interactions with Peptidoglycan Stem Peptide, Conquers Non-tuberculosis Mycobacteria.Journal of medicinal chemistry · 2023Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Drug resistant bacterial infections have emerged as one of the greatest threats to public health. The discovery and development of new antimicrobials and anti-infective strategies are urgently needed to address this challenge. Vancomycin is one of the most important antibiotics for the treatment of Gram-positive infections. Here, we introduce the vancomycin-arginine conjugate (V-R) as a highly effective antimicrobial against actively growing mycobacteria and difficult-to-treat mycobacterial biofilm populations. Further improvement in efficacy through combination treatment of V-R to inhibit peptidoglycan synthesis and ethambutol to inhibit arabinogalactan synthesis underscores the ability to identify compound synergies to more effectively target the Achilles heel of the cell-wall assembly. Moreover, we introduce mechanistic activity data and a molecular model derived from a d-Ala-d-Ala-bound vancomycin structure that we hypothesize underlies the molecular basis for the antibacterial improvement attributed to the arginine modification that is specific to peptidoglycan chemistry employed by mycobacteria and distinct from Gram-positive pathogens.
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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.