ArticleACS medicinal chemistry letters2012
Biotin analogues with antibacterial activity are potent inhibitors of biotin protein ligase.
Article in ACS medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 47 citations in OpenAlex.
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- Fighting Antimicrobial Resistance: Innovative Drugs in Antibacterial Research.Angewandte Chemie (International ed. in English) · 2025Review
- New Potent Sulfonamide-Based Inhibitors ofACS medicinal chemistry letters · 2024Article
- An environment-friendly methodology for the construction of diversified bicycloacenaphtho[1,2-d]imidazole-8-thione scaffolds using spinel NiFeMolecular diversity · 2022Article
- An Artificial Metalloenzyme Based on a Copper Heteroscorpionate Enables spJournal of the American Chemical Society · 2022Article
- Identification of Putative Vaccine and Drug Targets against the Methicillin-ResistantMolecules (Basel, Switzerland) · 2022Article
- Multiple Ehrlichia chaffeensis Genes Critical for Its Persistent Infection in a Vertebrate Host Are Identified by Random Mutagenesis Coupled withInfection and immunity · 2020Article
- Advanced Resistance Studies Identify Two Discrete Mechanisms inAntibiotics (Basel, Switzerland) · 2020Article
- The Biotin Biosynthetic Pathway in Mycobacterium tuberculosis is a Validated Target for the Development of Antibacterial Agents.Current medicinal chemistry · 2020Review
- AFrontiers in microbiology · 2020Article
- A Novel Lipoate-Protein Ligase, Mhp-LplJ, Is Required for Lipoic Acid Metabolism inFrontiers in microbiology · 2020Article
- Avoiding Antibiotic Inactivation in Mycobacterium tuberculosis by Rv3406 through Strategic Nucleoside Modification.ACS infectious diseases · 2018Article
- New Series of BPL Inhibitors To Probe the Ribose-Binding Pocket ofACS medicinal chemistry letters · 2016Article
- Chloromethyl-triazole: a new motif for site-selective pseudo-acylation of proteins.Chemical communications (Cambridge, England) · 2016Article
- Biotin Protein Ligase Is a Target for New Antibacterials.Antibiotics (Basel, Switzerland) · 2016Review
- The Mechanistic Targets of Antifungal Agents: An Overview.Mini reviews in medicinal chemistry · 2016Review
- Targeting Mycobacterium tuberculosis Biotin Protein Ligase (MtBPL) with Nucleoside-Based Bisubstrate Adenylation Inhibitors.Journal of medicinal chemistry · 2015Article
- Improved Synthesis of Biotinol-5'-AMP: Implications for Antibacterial Discovery.ACS medicinal chemistry letters · 2015Article
- Bisubstrate Inhibitors of Biotin Protein Ligase inACS medicinal chemistry letters · 2013Article
- Structural characterization of Staphylococcus aureus biotin protein ligase and interaction partners: an antibiotic target.Protein science : a publication of the Protein Society · 2013Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
There is a desperate need to develop new antibiotic agents to combat the rise of drug-resistant bacteria, such as clinically important Staphylococcus aureus. The essential multifunctional enzyme, biotin protein ligase (BPL), is one potential drug target for new antibiotics. We report the synthesis and characterization of a series of biotin analogues with activity against BPLs from S. aureus, Escherichia coli, and Homo sapiens. Two potent inhibitors with K i < 100 nM were identified with antibacterial activity against a panel of clinical isolates of S. aureus (MIC 2-16 μg/mL). Compounds with high ligand efficiency and >20-fold selectivity between the isozymes were identified and characterized. The antibacterial mode of action was shown to be via inhibition of BPL. The bimolecular interactions between the BPL and the inhibitors were defined by surface plasmon resonance studies and X-ray crystallography. These findings pave the way for second-generation inhibitors and antibiotics with greater potency and selectivity.
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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.