ArticleBioorganic & medicinal chemistry letters2010
Small molecule functional analogs of peptides that inhibit lambda site-specific recombination and bind Holliday junctions.
Article in Bioorganic & medicinal chemistry letters, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 22 citations in OpenAlex.
- Recent progress in probing small molecule interactions with DNA.Biophysical reviews · 2025Review
- Synthesis of Diazacyclic and Triazacyclic Small-Molecule Libraries Using Vicinal Chiral Diamines Generated from Modified Short Peptides and Their Application for Drug Discovery.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Interactions of small molecules with DNA junctions.Nucleic acids research · 2022Review
- Combinatorial Libraries As a Tool for the Discovery of Novel, Broad-Spectrum Antibacterial Agents Targeting the ESKAPE Pathogens.Journal of medicinal chemistry · 2015Article
- The λ Integrase Site-specific Recombination Pathway.Microbiology spectrum · 2015Review
- Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis.Journal of medicinal chemistry · 2014Article
- Scaffold ranking and positional scanning utilized in the discovery of nAChR-selective compounds suitable for optimization studies.Journal of medicinal chemistry · 2013Article
- The mathematics of a successful deconvolution: a quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors.Molecules (Basel, Switzerland) · 2013Article
- wrwyrggrywrw is a single-chain functional analog of the Holliday junction-binding homodimer, (wrwycr)2.Peptides · 2013Article
- HTS by NMR of combinatorial libraries: a fragment-based approach to ligand discovery.Chemistry & biology · 2013Article
- Tumor cell death mediated by peptides that recognize branched intermediates of DNA replication and repair.PloS one · 2013Article
- Similarities between exogenously- and endogenously-induced envelope stress: the effects of a new antibacterial molecule, TPI1609-10.PloS one · 2012Article
- Potent antimicrobial small molecules screened as inhibitors of tyrosine recombinases and Holliday junction-resolving enzymes.Molecular diversity · 2011Article
- Short peptides modulate the effect of endonucleases of wheat seedling.Doklady. Biochemistry and biophysicsArticle
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Our lab has isolated hexameric peptides that are structure-selective ligands of Holliday junctions (HJ), central intermediates of several DNA recombination reactions. One of the most potent of these inhibitors, WRWYCR, has shown antibacterial activity in part due to its inhibition of DNA repair proteins. To increase the therapeutic potential of these inhibitors, we searched for small molecule inhibitors with similar activities. We screened 11 small molecule libraries comprising over nine million individual compounds and identified a potent N-methyl aminocyclic thiourea inhibitor that also traps HJs formed during site-specific recombination reactions in vitro. This inhibitor binds specifically to protein-free HJs and can inhibit HJ resolution by RecG helicase, but only showed modest growth inhibition of bacterial with a hyperpermeable outer membrane; nonetheless, this is an important step in developing a functional analog of the peptide inhibitors.
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Registered trials
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