ArticleNature communications2019
Discovery of a chemical probe for PRDM9.
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Article in Nature communications, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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21citing papers in PubMed
3.0field-weighted citation impact, top 8% of its field
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Who cites it
21 citing papers in PubMed, 43 citations in OpenAlex.
- Identification and optimization of first-in-class RNA helicase inhibitors of DDX1, LGP2, and MDA5.European journal of medicinal chemistry · 2026Article
- PRDM Proteins Orchestrate Colorectal Cancer Tumorigenesis.International journal of molecular sciences · 2026Review
- Assembling Ternary Dead-End Complex for Covalent Trapping of Protein Lysine Methyltransferases.Journal of the American Chemical Society · 2026Article
- Histone methyltransferase PRDM9 promotes survival of drug-tolerant persister cells in glioblastoma.Nature communications · 2025Article
- Active Learning-Guided Hit Optimization for the Leucine-Rich Repeat Kinase 2 WDR Domain Based on In Silico Ligand-Binding Affinities.Journal of chemical information and modeling · 2025Article
- Lysine and arginine methylation of transcription factors.Cellular and molecular life sciences : CMLS · 2024Review
- Comparative study of machine-and deep-learning based classification algorithms for biomedical Raman spectroscopy (RS): case study of RS based pathogenic microbe identification.Analytical sciences : the international journal of the Japan Society for Analytical Chemistry · 2024Article
- Cancer testis antigens: Emerging therapeutic targets leveraging genomic instability in cancer.Molecular therapy. Oncology · 2024Review
- Targeting Alpha-Ketoglutarate Disruption Overcomes Immunoevasion and Improves PD-1 Blockade Immunotherapy in Renal Cell Carcinoma.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2023Article
- Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2).Journal of medicinal chemistry · 2023Review
- Target 2035 - an update on private sector contributions.RSC medicinal chemistry · 2023Article
- A specific G9a inhibitor unveils BGLT3 lncRNA as a universal mediator of chemically induced fetal globin gene expression.Nature communications · 2023Article
- Lysine methyltransferase inhibitors: where we are now.RSC chemical biology · 2022Review
- The duality of PRDM proteins: epigenetic and structural perspectives.The FEBS journal · 2022Review
- A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization.Nature chemical biology · 2022Article
- Meiotic Genes and DNA Double Strand Break Repair in Cancer.Frontiers in genetics · 2022Review
- New Wenshen Shengjing Decoction Improves Early Embryonic Development by Maintaining Low Levels of H3K4me3 in Sperm.BioMed research international · 2022Article
- Review
- Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease.Nature reviews. Drug discovery · 2021Review
- Multifaceted Role of PRDM Proteins in Human Cancer.International journal of molecular sciences · 2020Review
Corrections and comments
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Authors and funding
30 authors at 3 institutions in 4 countries.
Abdellah Allali-HassaniStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.
Magdalena M SzewczykStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.
Danton IvanochkoStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.
Shawna L OrganStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.
Jabez BokInstitute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore.
Jessica Sook Yuin HoInstitute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore.ORCID http://orcid.org/0000-0003-2234-2602
Florence P H GayInstitute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore.
Fengling LiStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.
Levi BlazerStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.
Mohammad S EramStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.
Levon HalabelianStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.ORCID http://orcid.org/0000-0003-4361-3619
David DilworthStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.ORCID http://orcid.org/0000-0001-5557-9476
Genna M LucianiStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.ORCID http://orcid.org/0000-0001-8107-2708
Evelyne Lima-FernandesStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.ORCID http://orcid.org/0000-0002-3628-9745
Qin WuStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.
Peter LoppnauStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.
Nathan PalmerInstitute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore.
S Zakiah A TalibInstitute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore.ORCID http://orcid.org/0000-0002-6063-254X
Peter J BrownStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.ORCID http://orcid.org/0000-0002-8454-0367
Matthieu SchapiraStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.ORCID http://orcid.org/0000-0002-1047-3309
Philipp KaldisInstitute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore.ORCID http://orcid.org/0000-0002-7247-7591
Ronan C O'HaganMerck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ, 07033, USA.
Ernesto GuccioneInstitute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR), Singapore, Singapore.
Dalia Barsyte-LovejoyStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.ORCID http://orcid.org/0000-0002-6560-9621
Cheryl H ArrowsmithStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada.ORCID http://orcid.org/0000-0002-4971-3250
John M SandersMerck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ, 07033, USA.ORCID http://orcid.org/0000-0002-3788-4220
Solomon D KattarMerck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ, 07033, USA.
D Jonathan BennettMerck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ, 07033, USA.ORCID http://orcid.org/0000-0003-0163-7479
Benjamin NicholsonMerck & Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ, 07033, USA. benjamin.nicholson@merck.com.
Masoud VedadiStructural Genomics Consortium, University of Toronto, Toronto, ON, M5G 1L7, Canada. m.vedadi@utoronto.ca.ORCID http://orcid.org/0000-0002-0574-0169
University of Toronto · CAAgency for Science, Technology and Research · SGMerck & Co., Inc., Rahway, NJ, USA (United States) · US
Funding
Wellcome Trust
Abstract
PRDM9 is a PR domain containing protein which trimethylates histone 3 on lysine 4 and 36. Its normal expression is restricted to germ cells and attenuation of its activity results in altered meiotic gene transcription, impairment of double-stranded breaks and pairing between homologous chromosomes. There is growing evidence for a role of aberrant expression of PRDM9 in oncogenesis and genome instability. Here we report the discovery of MRK-740, a potent (IC
Indexed as
Crystallography, X-RayDNA MethylationDrug DiscoveryEnzyme InhibitorsHEK293 CellsHistone-Lysine N-MethyltransferaseHistonesHumansInhibitory Concentration 50Molecular Dynamics SimulationMolecular ProbesProtein DomainsS-AdenosylmethionineEnzyme Inhibitorshistone H3 trimethyl Lys4Histone-Lysine N-MethyltransferaseHistonesMolecular ProbesPRDM9 protein, humanS-Adenosylmethionine
Identifiers
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LicenceCC BY
Read underepoch 390
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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.