ArticleACS combinatorial science2020
Optimization of High-Throughput Methyltransferase Assays for the Discovery of Small Molecule Inhibitors.
Article in ACS combinatorial science, 2020. 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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Who cites it
17 citing papers in PubMed, 22 citations in OpenAlex.
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- Quinoline-based compounds can inhibit diverse enzymes that act on DNA.Cell chemical biology · 2024Article
- Closing in on human methylation-the versatile family of seven-β-strand (METTL) methyltransferases.Nucleic acids research · 2024Review
- Ocr-mediated suppression of BrxX unveils a phage counter-defense mechanism.Nucleic acids research · 2024Article
- A sequential one-pot approach for rapid and convenient characterization of putative restriction-modification systems.mSystems · 2023Article
- Effects of Oncohistone Mutations and PTM Crosstalk on the N-Terminal Acetylation Activities of NatD.ACS chemical biology · 2023Article
- Comparative Study of Adenosine Analogs as Inhibitors of Protein Arginine Methyltransferases and aACS chemical biology · 2023Article
- Venglustat Inhibits Protein N-Terminal Methyltransferase 1 in a Substrate-Competitive Manner.Journal of medicinal chemistry · 2022Article
- Structure, dynamics, and molecular inhibition of the Staphylococcus aureus mThe Journal of biological chemistry · 2022Article
- A Direct Assay for Measuring the Activity and Inhibition of Coactivator-Associated Arginine Methyltransferase 1.Biochemistry · 2022Article
- Mechanisms and inhibitors of nicotinamideRSC medicinal chemistry · 2021Review
- Clostridioides difficile specific DNA adenine methyltransferase CamA squeezes and flips adenine out of DNA helix.Nature communications · 2021Article
- Development of A Continuous Fluorescence-Based Assay forInternational journal of molecular sciences · 2021Article
- Enzymatic characterization of three human RNA adenosine methyltransferases reveals diverse substrate affinities and reaction optima.The Journal of biological chemistryArticle
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
Methyltransferases (MTases) play diverse roles in cellular processes. Aberrant methylation levels have been implicated in many diseases, indicating the need for the identification and development of small molecule inhibitors for each MTase. Specific inhibitors can serve as probes to investigate the function and validate therapeutic potential for the respective MTase. High-throughput screening (HTS) is a powerful method to identify initial hits for further optimization. Here, we report the development of a fluorescence-based MTase assay and compare this format with the recently developed MTase-Glo luminescence assay for application in HTS. Using protein N-terminal methyltransferase 1 (NTMT1) as a model system, we miniaturized to 1536-well quantitative HTS format. Through a pilot screen of 1428 pharmacologically active compounds and subsequent validation, we discovered that MTase-Glo produced lower false positive rates than the fluorescence-based MTase assay. Nevertheless, both assays displayed robust performance along with low reagent requirements and can potentially be employed as general HTS formats for the discovery of inhibitors for any MTase.
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