ArticleAntimicrobial agents and chemotherapy2006
Peptide deformylase inhibitors as potent antimycobacterial agents.
Article in Antimicrobial agents and chemotherapy, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 56 citations in OpenAlex.
- Ensemble learning-guided discovery of anti-tuberculosis phytochemicals: computational prediction and mechanistic insights.Journal of computer-aided molecular design · 2026Article
- Structures of Legionella pneumophila serogroup 1 peptide deformylase bound to nickel(II) and actinonin.Acta crystallographica. Section F, Structural biology communications · 2025Article
- Exploration of novel bioactive compounds from the microbiome of fish and shellfish as an alternative to replace antibiotic drugs in aquaculture farming.Gut microbiome (Cambridge, England) · 2025Review
- Blunted blades: new CRISPR-derived technologies to dissect microbial multi-drug resistance and biofilm formation.mSphere · 2024Review
- Cryosphere: a frozen home of microbes and a potential source for drug discovery.Archives of microbiology · 2024Review
- Antimicrobial Compounds from Microorganisms.Antibiotics (Basel, Switzerland) · 2022Review
- EfgA is a conserved formaldehyde sensor that leads to bacterial growth arrest in response to elevated formaldehyde.PLoS biology · 2021Article
- A Repurposing Approach for Uncovering the Anti-Tubercular Activity of FDA-Approved Drugs with Potential Multi-Targeting Profiles.Molecules (Basel, Switzerland) · 2019Article
- Peptide Deformylase (def) is essential in Mycobacterium smegmatis, but the essentiality is compensated by inactivation of methionine formylation.BMC microbiology · 2019Article
- Article
- The gene fmt, encoding tRNAScientific reports · 2017Article
- Identification of new drug targets and resistance mechanisms in Mycobacterium tuberculosis.PloS one · 2013Article
- Expression, purification, and activity assay of peptide deformylase from Escherichia coli and Staphylococcus aureus.Molecular and cellular biochemistry · 2011Article
- Structure and activity of human mitochondrial peptide deformylase, a novel cancer target.Journal of molecular biology · 2009Article
- Mutations in three distinct loci cause resistance to peptide deformylase inhibitors in Bacillus subtilis.Antimicrobial agents and chemotherapy · 2009Article
- Expression, crystallization and preliminary X-ray crystallographic analysis of peptide deformylase from Xanthomonas oryzae pv. oryzae.Acta crystallographica. Section F, Structural biology and crystallization communications · 2008Article
- Three consecutive arginines are important for the mycobacterial peptide deformylase enzyme activity.The Journal of biological chemistry · 2008Article
- Drug forecast - the peptide deformylase inhibitors as antibacterial agents.Therapeutics and clinical risk management · 2007Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
18 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Peptide deformylase (PDF) catalyzes the hydrolytic removal of the N-terminal formyl group from nascent proteins. This is an essential step in bacterial protein synthesis, making PDF an attractive target for antibacterial drug development. Essentiality of the def gene, encoding PDF from Mycobacterium tuberculosis, was demonstrated through genetic knockout experiments with Mycobacterium bovis BCG. PDF from M. tuberculosis strain H37Rv was cloned, expressed, and purified as an N-terminal histidine-tagged recombinant protein in Escherichia coli. A novel class of PDF inhibitors (PDF-I), the N-alkyl urea hydroxamic acids, were synthesized and evaluated for their activities against the M. tuberculosis PDF enzyme as well as their antimycobacterial effects. Several compounds from the new class had 50% inhibitory concentration (IC50) values of <100 nM. Some of the PDF-I displayed antibacterial activity against M. tuberculosis, including MDR strains with MIC90 values of <1 microM. Pharmacokinetic studies of potential leads showed that the compounds were orally bioavailable. Spontaneous resistance towards these inhibitors arose at a frequency of < or =5 x 10(-7) in M. bovis BCG. DNA sequence analysis of several spontaneous PDF-I-resistant mutants revealed that half of the mutants had acquired point mutations in their formyl methyltransferase gene (fmt), which formylated Met-tRNA. The results from this study validate M. tuberculosis PDF as a drug target and suggest that this class of compounds have the potential to be developed as novel antimycobacterial agents.
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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.