ReviewMolecules (Basel, Switzerland)2012
Development of new drugs for an old target: the penicillin binding proteins.
Review in Molecules (Basel, Switzerland), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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Who cites it
46 citing papers in PubMed.
- Giving Antibiotics a Second Chance: Evolutionary Trade-Offs and Phage-Driven Restoration of Antibiotic Susceptibility.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy · 2026Review
- Leak Proof PDBBind: A Reorganized Data Set of Protein-Ligand Complexes for More Generalizable Binding Affinity Prediction.The journal of physical chemistry. B · 2026Article
- Enzymatic Synthesis of β-lactam Antibiotics: From Enzyme Dataset Construction to Action Mechanism and Semi-Rational Design.Current protein & peptide science · 2026Review
- Boronate-Based Inhibitors of Penicillin-Binding Proteins: An Underestimated Avenue for Antibiotic Discovery?Pharmaceuticals (Basel, Switzerland) · 2025Article
- Synergistic potential of LeuBMC microbiology · 2024Article
- Rhodanine derived enethiols react to give 1,3-dithiolanes and mixed disulfides.RSC medicinal chemistry · 2024Article
- A Review on Five and Six-Membered Heterocyclic Compounds Targeting the Penicillin-Binding Protein 2 (PBP2A) of Methicillin-ResistantMolecules (Basel, Switzerland) · 2023Review
- Optimizing the Use of Beta-Lactam Antibiotics in Clinical Practice: A Test of Time.Open forum infectious diseases · 2023Article
- Development of novel isatin thiazolyl-pyrazoline hybrids as promising antimicrobials in MDR pathogens.RSC advances · 2022Article
- Chelation in Antibacterial Drugs: From Nitroxoline to Cefiderocol and Beyond.Antibiotics (Basel, Switzerland) · 2022Review
- Macromolecular Structure Assembly as a Novel Antibiotic Target.Antibiotics (Basel, Switzerland) · 2022Article
- Peptidoglycan biosynthesis is driven by lipid transfer along enzyme-substrate affinity gradients.Nature communications · 2022Article
- β-LacFamPred: An online tool for prediction and classification of β-lactamase class, subclass, and family.Frontiers in microbiology · 2022Article
- Enzyme Inhibitors: The Best Strategy to Tackle Superbug NDM-1 and Its Variants.International journal of molecular sciences · 2021Review
- The Effect of Rotating Magnetic Field on Susceptibility Profile of Methicillin-ResistantInternational journal of molecular sciences · 2021Article
- Interaction Mode of the Novel Monobactam AIC499 Targeting Penicillin Binding Protein 3 of Gram-Negative Bacteria.Biomolecules · 2021Article
- The penicillin binding protein 1A of Helicobacter pylori, its amoxicillin binding site and access routes.Gut pathogens · 2021Article
- Article
- Significant increase in the secretion of extracellular vesicles and antibiotics resistance from methicillin-resistant Staphylococcus aureus induced by ampicillin stress.Scientific reports · 2020Article
- Recent advances in the development of β-lactamase inhibitors.Journal of microbiology (Seoul, Korea) · 2020Review
Corrections and comments
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The widespread use of β-lactam antibiotics has led to the worldwide appearance of drug-resistant strains. Bacteria have developed resistance to β-lactams by two main mechanisms: the production of β-lactamases, sometimes accompanied by a decrease of outer membrane permeability, and the production of low-affinity, drug resistant Penicillin Binding Proteins (PBPs). PBPs remain attractive targets for developing new antibiotic agents because they catalyse the last steps of the biosynthesis of peptidoglycan, which is unique to bacteria, and lies outside the cytoplasmic membrane. Here we summarize the “current state of the art” of non-β-lactam inhibitors of PBPs, which have being developed in an attempt to counter the emergence of β-lactam resistance. These molecules are not susceptible to hydrolysis by β-lactamases and thus present a real alternative to β-lactams. We present transition state analogs such as boronic acids, which can covalently bind to the active serine residue in the catalytic site. Molecules containing ring structures different from the β-lactam-ring like lactivicin are able to acylate the active serine residue. High throughput screening methods, in combination with virtual screening methods and structure based design, have allowed the development of new molecules. Some of these novel inhibitors are active against major pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and thus open avenues new for the discovery of novel antibiotics.
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