ArticleJournal of medicinal chemistry2018
Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).
Open access · greenAbstract read
In one paragraph
Article in Journal of medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
0numbers the graph read from it
0cells of the map it votes in
27citing papers in PubMed
1.5field-weighted citation impact, top 18% of its field
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
27 citing papers in PubMed, 39 citations in OpenAlex.
- Protein arginine methyltransferases as metabolic regulators: many roles beyond cancer.Science China. Life sciences · 2026Review
- Article
- Discovery of a potent and orally bioavailable type Ⅰ PRMTs inhibitor for triple-negative breast cancer treatment.Acta pharmacologica Sinica · 2026Article
- Synthesis, characterization, and α-glucosidase inhibitory activity of methyl proline derivatives of phenylpropanoid.RSC advances · 2026Article
- PRMT3 in cancer: arginine methylation as a driver of tumor metabolism, immune evasion, and therapeutic resistance.Frontiers in immunology · 2026Review
- Current and Emerging Therapies for Targeting Protein Arginine Methyltransferases (PRMTs) in Cancer.International journal of molecular sciences · 2025Review
- General Approach To Access Aldehyde Oxidase Metabolites of Drug Molecules viaOrganic letters · 2025Article
- PRMT3 reverses HIV-1 latency by increasing chromatin accessibility to form a TEAD4-P-TEFb-containing transcriptional hub.Nature communications · 2025Article
- PRMT3 drives PD-L1-mediated immune escape through activating PDHK1-regulated glycolysis in hepatocellular carcinoma.Cell death & disease · 2025Article
- PRMT3 at the crossroads of inflammation: dual roles in metabolic reprogramming and immune dysregulation in chronic diseases.Frontiers in immunology · 2025Review
- Discovery of PRMT3 Degrader for the Treatment of Acute Leukemia.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Access to pyrrolines and fused diaziridines by selective radical addition to homoallylic diazirines.Chemical science · 2024Article
- Article
- Identification and Inhibition of the Druggable Allosteric Site of SARS-CoV-2 NSP10/NSP16 Methyltransferase through Computational Approaches.Molecules (Basel, Switzerland) · 2022Article
- Naturally occurring cancer-associated mutations disrupt oligomerization and activity of protein arginine methyltransferase 1 (PRMT1).The Journal of biological chemistry · 2021Article
- Discovery of a potent and dual-selective bisubstrate inhibitor for protein arginine methyltransferase 4/5.Acta pharmaceutica Sinica. B · 2021Article
- A Pan-Inhibitor for Protein Arginine Methyltransferase Family Enzymes.Biomolecules · 2021Article
- Review
- Naegleria fowleri: Protein structures to facilitate drug discovery for the deadly, pathogenic free-living amoeba.PloS one · 2021Article
- Allosteric Modulation of Protein Arginine Methyltransferase 5 (PRMT5).ACS medicinal chemistry letters · 2020Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
27 authors at 5 institutions in 3 countries.
H Ümit KaniskanCenter for Chemical Biology and Drug Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.
Mohammad S EramStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.
Kehao ZhaoNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
Magdalena M SzewczykStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.
Xiaobao YangCenter for Chemical Biology and Drug Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.
Keith SchmidtCenter for Chemical Biology and Drug Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.
Xiao LuoNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
Sean XiaoNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
Miao DaiNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
Feng HeNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
Irene ZangNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
Ying LinNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
Fengling LiStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.
Elena DobrovetskyStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.
David SmilStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.
Sun-Joon MinCenter for Chemical Biology and Drug Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.ORCID 0000-0003-0867-4416
Jennifer Lin-JonesDiscoveRx Corporation , Fremont, California 94538, United States.
Matthieu SchapiraStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.ORCID 0000-0002-1047-3309
Peter AtadjaNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
En LiNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
Dalia Barsyte-LovejoyStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.
Cheryl H ArrowsmithStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.ORCID 0000-0002-4971-3250
Peter J BrownStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.
Feng LiuJiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases and Department of Medicinal Chemistry, College of Pharmaceutical Sciences, Soochow University , Suzhou, Jiangsu 215123, China.ORCID 0000-0003-2669-5448
Zhengtian YuNovartis Institutes for Biomedical Research (China), Zhangjiang Hi-Tech Park , Pudong New Area, Shanghai 201203, China.
Masoud VedadiStructural Genomics Consortium, University of Toronto , Toronto, ON M5G 1L7, Canada.
Jian JinCenter for Chemical Biology and Drug Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai , New York, New York 10029, United States.ORCID 0000-0002-2387-3862
Novartis (China) · CNUniversity of Toronto · CAIcahn School of Medicine at Mount Sinai · USDiscoveRx (United States) · USSoochow University · CN
Funding
Epigenetic Therapy and Prader-Willi SyndromeR01HD088626 · NICHD · YALE UNIVERSITY · PI JIANG, YONG-HUI, JIN, JIAN · 2017 to 2021
$2.8MTargeting Lysine Methyltransferases EZH2 and EZH1 for Treating MLL-rearranged LeukemiasR01CA218600 · NCI · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI JIN, JIAN, WANG, G GREG · 2017 to 2021
$2.8MDiscovery of Selective Inhibitors for Histone MethyltransferasesR01GM122749 · NIGMS · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI JIN, JIAN · 2017 to 2020
$1.3MNCI NIH HHS R01 CA218600NICHD NIH HHS R01 HD088626NIGMS NIH HHS R01 GM122749Wellcome Trust
Abstract
PRMT3 catalyzes the asymmetric dimethylation of arginine residues of various proteins. It is crucial for maturation of ribosomes and has been implicated in several diseases. We recently disclosed a highly potent, selective, and cell-active allosteric inhibitor of PRMT3, compound 4. Here, we report comprehensive structure-activity relationship studies that target the allosteric binding site of PRMT3. We conducted design, synthesis, and evaluation of novel compounds in biochemical, selectivity, and cellular assays that culminated in the discovery of 4 and other highly potent (IC
Indexed as
Drug DesignAllosteric RegulationBridged Bicyclo Compounds, HeterocyclicHEK293 CellsHumansHydrogen BondingInhibitory Concentration 50Models, MolecularProtein-Arginine N-MethyltransferasesProtein ConformationStructure-Activity RelationshipBridged Bicyclo Compounds, HeterocyclicPRMT3 protein, humanProtein-Arginine N-Methyltransferases
Identifiers
What OpenQuestion holds
Textmetadata
Read underepoch 390
Registered trials
None linked
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.