ArticleACS chemical biology2012
Novel inhibitors for PRMT1 discovered by high-throughput screening using activity-based fluorescence polarization.
Article in ACS chemical biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
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
28 citing papers in PubMed.
- Structure of the Beat-Side complex reveals their interaction is required for neuromuscular system wiring.Cell reports · 2026Article
- PRMT1-Mediated SWI/SNF Complex Recruitment via SMARCC1 Drives IGF2BP2 Transcription to Enhance Carboplatin Resistance in Head and Neck Squamous Cell Carcinoma.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Activity-Based Profiling of Retaining Glycosidases in Disease Diagnosis and Their Application in Drug Discovery.Handbook of experimental pharmacology · 2025Review
- miR-455-5p promotes pathological cardiac remodeling via suppression of PRMT1-mediated Notch signaling pathway.Cellular and molecular life sciences : CMLS · 2023Article
- A super-enhancer-regulated RNA-binding protein cascade drives pancreatic cancer.Nature communications · 2023Article
- 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
- Structural and biochemical evaluation of bisubstrate inhibitors of protein arginine N-methyltransferases PRMT1 and CARM1 (PRMT4).The Biochemical journal · 2020Article
- Direct and Indirect Targeting of HOXA9 Transcription Factor in Acute Myeloid Leukemia.Cancers · 2019Review
- Epigenetic Therapies for Acute Myeloid Leukemia and Their Immune-Related Effects.Frontiers in cell and developmental biology · 2019Review
- PRMT1 Plays a Critical Role in Th17 Differentiation by Regulating Reciprocal Recruitment of STAT3 and STAT5.Journal of immunology (Baltimore, Md. : 1950) · 2018Article
- Targeting Transcription Factors for Cancer Treatment.Molecules (Basel, Switzerland) · 2018Review
- Inhibitors of Protein Methyltransferases and Demethylases.Chemical reviews · 2018Review
- Protein arginine methylation: an emerging regulator of the cell cycle.Cell division · 2018Review
- Reactive oxygen species extend insect life span using components of the insulin-signaling pathway.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- PubChem BioAssay: A Decade's Development toward Open High-Throughput Screening Data Sharing.SLAS discovery : advancing life sciences R & D · 2017Article
- Root morphogenic pathways in Eucalyptus grandis are modified by the activity of protein arginine methyltransferases.BMC plant biology · 2017Article
- Pharmacologic Targeting of Chromatin Modulators As Therapeutics of Acute Myeloid Leukemia.Frontiers in oncology · 2017Review
- Protein arginine methyltransferase 1 promoted the growth and migration of cancer cells in esophageal squamous cell carcinoma.Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine · 2016Article
- Cluster analysis ofF1000Research · 2016Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
Protein arginine methyltransferases (PRMTs) catalyze the posttranslational methylation of arginine using S-adenosylmethionine (SAM) as a methyl-donor. The PRMT family is widely expressed and has been implicated in biological functions such as RNA splicing, transcriptional control, signal transduction, and DNA repair. Therefore, specific inhibitors of individual PRMTs have potentially significant research and therapeutic value. In particular, PRMT1 is responsible for >85% of arginine methyltransferase activity, but currently available inhibitors of PRMT1 lack specificity, efficacy, and bioavailability. To address this limitation, we developed a high-throughput screening assay for PRMT1 that utilizes a hyper-reactive cysteine within the active site, which is lacking in almost all other PRMTs. This assay, which monitors the kinetics of the fluorescence polarization signal increase upon PRMT1 labeling by a rhodamine-containing cysteine-reactive probe, successfully identified two novel inhibitors selective for PRMT1 over other SAM-dependent methyltransferases.
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Registered trials
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.