ArticleJournal of biomolecular screening2012
Development and validation of a generic fluorescent methyltransferase activity assay based on the transcreener AMP/GMP assay.
Article in Journal of biomolecular screening, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
13 citing papers in PubMed.
- The emerging role of CARM1 in cancer.Cellular oncology (Dordrecht, Netherlands) · 2024Review
- Development and validation of a generic methyltransferase enzymatic assay based on an SAH riboswitch.SLAS discovery : advancing life sciences R & D · 2024Article
- Chemical probes and methods for the study of protein arginine methylation.RSC chemical biology · 2023Review
- A sensitive homogeneous enzyme assay for euchromatic histone-lysine-N-methyltransferase 2 (G9a) based on terbium-to-quantum dot time-resolved FRET.BioImpacts : BI · 2021Article
- Direct Detection of Products from S-Adenosylmethionine-Dependent Enzymes Using a Competitive Fluorescence Polarization Assay.Analytical chemistry · 2018Article
- A simplified characterization ofChemical science · 2017Article
- Epigenetic assays for chemical biology and drug discovery.Clinical epigenetics · 2017Review
- In Vitro and In Vivo Enzyme Activity Screening via RNA-Based Fluorescent Biosensors for S-Adenosyl-l-homocysteine (SAH).Journal of the American Chemical Society · 2016Article
- Development, validation and quantitative assessment of an enzymatic assay suitable for small molecule screening and profiling: A case-study.Biomolecular detection and quantification · 2015Article
- A continuous kinetic assay for protein and DNA methyltransferase enzymatic activities.Epigenetics & chromatin · 2015Article
- A sensitive luminescent assay for the histone methyltransferase NSD1 and other SAM-dependent enzymes.Assay and drug development technologies · 2014Article
- Taking a bite: endocytosis in the maintenance of the slit diaphragm.The Journal of clinical investigation · 2012Article
- Current chemical biology approaches to interrogate protein methyltransferases.ACS chemical biology · 2012Review
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Methylation is a ubiquitous covalent modification used to control the function of diverse biomolecules including hormones, neurotransmitters, xenobiotics, proteins, nucleic acids, and lipids. Histone methyltransferases (HMTs) are currently of high interest as drug targets because of their role in epigenetic regulation; however, most HMT assay methods are either not amenable to a high-throughput screening (HTS) environment or are applicable to a limited number of enzymes. The authors developed a generic methyltransferase assay method using fluorescent immunodetection of adenosine monophosphate (AMP), which is formed from the MT reaction product S-adenosylhomocysteine in a dual-enzyme coupling step. The detection range of the assay; its suitability for HTS, including stability of reagents following dispensing and after addition to reactions; and the potential for interference from drug-like molecules was investigated. In addition, the use of the assay for measuring inhibitor potencies with peptide or intact protein substrates was examined through pilot screening with selected reference enzymes including HMT G9a. By combining a novel enzymatic coupling step with the well-characterized Transcreener AMP/GMP assay, the authors have developed a robust HTS assay for HMTs that should be broadly applicable to other types of methyltransferases as well.
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Registered trials
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