ArticleNature communications2022
Synthesis of macrocyclic nucleoside antibacterials and their interactions with MraY.
Article in Nature communications, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed.
- Designing the Next Generation of Antibiotics: Structure, SAR, and Strategy in Medicinal Chemistry (2000-2025).Medicinal research reviews · 2026Review
- Structures of Bacterial and Human Phosphoglycosyltransferases Bound to a Common Inhibitor Inform Selective Therapeutics.ACS chemical biology · 2026Article
- A metal-aware library-expansion and virtual-screening workflow forFrontiers in microbiology · 2026Article
- Predictive Factors for Upper Urinary Tract Stones Combined with Carbapenem-Resistant Enterobacteriaceae Associated Urinary Tract Infections.Infection and drug resistance · 2026Article
- 1,2,4-Triazole-Based First-in-Class Non-Nucleoside Inhibitors of the Bacterial Enzyme MraY.ACS bio & med chem Au · 2025Article
- Structures of bacterial and human phosphoglycosyltransferases bound to a common inhibitor inform selective therapeutics.bioRxiv : the preprint server for biology · 2025Article
- Advances in Coordination Chemistry of Schiff Base Complexes: A Journey from Nanoarchitectonic Design to Biomedical Applications.Topics in current chemistry (Cham) · 2025Review
- Identifying Opportunity Targets in Gram-Negative Pathogens for Infectious Disease Mitigation.ACS central science · 2025Review
- Computational prediction of CNP0387675 as a non-nucleoside inhibitor of MraY, from natural product-based multi-template screening againstFrontiers in microbiology · 2025Article
- Development of a natural product optimization strategy for inhibitors against MraY, a promising antibacterial target.Nature communications · 2024Article
- Unrealized targets in the discovery of antibiotics for Gram-negative bacterial infections.Nature reviews. Drug discovery · 2023Review
- A review of current antibiotic resistance and promising antibiotics with novel modes of action to combat antibiotic resistance.Archives of microbiology · 2023Review
- Structure-Based Insight on the Mechanism of N-Glycosylation Inhibition by Tunicamycin.Molecules and cells · 2023Review
- An Update Review of Approaches to Multiple Action-Based Antibacterials.Antibiotics (Basel, Switzerland) · 2023Review
- Article
- Computational Approaches to Enzyme Inhibition by Marine Natural Products in the Search for New Drugs.Marine drugs · 2023Review
- The challenges and opportunities of developing small molecule inhibitors of MraY.Annual reports in medicinal chemistry · 2023Article
Corrections and comments
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Authors and funding
14 authors.
Funding
Abstract
The development of new antibacterial drugs with different mechanisms of action is urgently needed to address antimicrobial resistance. MraY is an essential membrane enzyme required for bacterial cell wall synthesis. Sphaerimicins are naturally occurring macrocyclic nucleoside inhibitors of MraY and are considered a promising target in antibacterial discovery. However, developing sphaerimicins as antibacterials has been challenging due to their complex macrocyclic structures. In this study, we construct their characteristic macrocyclic skeleton via two key reactions. Having then determined the structure of a sphaerimicin analogue bound to MraY, we use a structure-guided approach to design simplified sphaerimicin analogues. These analogues retain potency against MraY and exhibit potent antibacterial activity against Gram-positive bacteria, including clinically isolated drug resistant strains of S. aureus and E. faecium. Our study combines synthetic chemistry, structural biology, and microbiology to provide a platform for the development of MraY inhibitors as antibacterials against drug-resistant 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.