ArticleMolecular bioSystems2011
Formulating a fluorogenic assay to evaluate S-adenosyl-L-methionine analogues as protein methyltransferase cofactors.
Article in Molecular bioSystems, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 44 citations in OpenAlex.
- Assembling Ternary Dead-End Complex for Covalent Trapping of Protein Lysine Methyltransferases.Journal of the American Chemical Society · 2026Article
- Chemical probes and methods for the study of protein arginine methylation.RSC chemical biology · 2023Review
- Molecular probes for cellular imaging of post-translational proteoforms.RSC chemical biology · 2022Review
- Profiling and Validation of Live-Cell Protein Methylation with Engineered Enzymes and Methionine Analogues.Current protocols · 2021Article
- Molecular Epigenetics: Chemical Biology Tools Come of Age.Annual review of biochemistry · 2021Review
- Mechanisms and Inhibitors of Histone Arginine Methylation.Chemical record (New York, N.Y.) · 2018Review
- Chemical and Biochemical Perspectives of Protein Lysine Methylation.Chemical reviews · 2018Review
- Methyltransferase-Directed Labeling of Biomolecules and its Applications.Angewandte Chemie (International ed. in English) · 2017Review
- Epigenetic assays for chemical biology and drug discovery.Clinical epigenetics · 2017Review
- AdoMet analog synthesis and utilization: current state of the art.Current opinion in biotechnology · 2016Review
- 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
- SAM/SAH Analogs as Versatile Tools for SAM-Dependent Methyltransferases.ACS chemical biology · 2016Review
- Small Molecule Inhibitors of Protein Arginine Methyltransferases.Expert opinion on investigational drugs · 2016Review
- Redox Control of Protein Arginine Methyltransferase 1 (PRMT1) Activity.The Journal of biological chemistry · 2015Article
- Emerging technologies to map the protein methylome.Journal of molecular biology · 2014Review
- A sensitive luminescent assay for the histone methyltransferase NSD1 and other SAM-dependent enzymes.Assay and drug development technologies · 2014Article
- A sensitive mass spectrum assay to characterize engineered methionine adenosyltransferases with S-alkyl methionine analogues as substrates.Analytical biochemistry · 2014Article
- Profiling substrates of protein arginine N-methyltransferase 3 with S-adenosyl-L-methionine analogues.ACS chemical biology · 2014Article
- A journey toward Bioorthogonal Profiling of Protein Methylation inside living cells.Current opinion in chemical biology · 2013Review
- Bioorthogonal profiling of protein methylation (BPPM) using an azido analog of S-adenosyl-L-methionine.Current protocols in chemical biology · 2013Article
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7 authors at 1 institution in 1 country.
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Abstract
Protein methyltransferases (PMTs) catalyze arginine and lysine methylation of diverse histone and nonhistone targets. These posttranslational modifications play essential roles in regulating multiple cellular events in an epigenetic manner. In the recent process of defining PMT targets, S-adenosyl-L-methionine (SAM) analogues have emerged as powerful small molecule probes to label and profile PMT targets. To examine efficiently the reactivity of PMTs and their variants on SAM analogues, we transformed a fluorogenic PMT assay into a ready high throughput screening (HTS) format. The reformulated fluorogenic assay is featured by its uncoupled but more robust character with the first step of accumulation of the commonly-shared reaction byproduct S-adenosyl-L-homocysteine (SAH), followed by SAH-hydrolase-mediated fluorogenic quantification. The HTS readiness and robustness of the assay were demonstrated by its excellent Z' values of 0.83-0.95 for the so-far-examined 8 human PMTs with SAM as a cofactor (PRMT1, PRMT3, CARM1, SUV39H2, SET7/9, SET8, G9a and GLP1). The fluorogenic assay was further implemented to screen the PMTs against five SAM analogues (allyl-SAM, propargyl-SAM, (E)-pent-2-en-4-ynyl-SAM (EnYn-SAM), (E)-hex-2-en-5-ynyl-SAM (Hey-SAM) and 4-propargyloxy-but-2-enyl-SAM (Pob-SAM)). Among the examined 8 × 5 pairs of PMTs and SAM analogues, native SUV39H2, G9a and GLP1 showed promiscuous activity on allyl-SAM. In contrast, the bulky SAM analogues, such as EnYn-SAM, Hey-SAM and Pob-SAM, are inert toward the panel of human PMTs. These findings therefore provide the useful structure-activity guidance to further evolve PMTs and SAM analogues for substrate labeling. The current assay format is ready to screen methyltransferase variants on structurally-diverse SAM analogues.
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