ArticleJournal of medicinal chemistry2022
Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
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Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
0numbers the graph read from it
0cells of the map it votes in
44citing papers in PubMed
6.8field-weighted citation impact, top 2% of its field
What it found
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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
44 citing papers in PubMed, 65 citations in OpenAlex.
- Bevacizumab induces apoptosis in glioblastoma cells by upregulating miR-4695-5p to inhibit PKMYT1.RNA biology · 2026Article
- Article
- Design, Synthesis, Biological Activity Evaluation, and Molecular Docking of 2-Aminopyrimidine-Based PKMYT1 Inhibitors.Biomedicines · 2026Article
- Phenols: From Replacing to Embracing.ChemMedChem · 2026Review
- 7-azaindole as privileged scaffold: Advances in drug design and structural modification.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- PKMYT1 in Cancer: Beyond Cell Cycle Checkpoints to Context-Dependent Therapeutic Vulnerability.Genes, chromosomes & cancer · 2026Review
- Synthetic lethality in cancer: mechanism exploration and therapeutic applications.Cell communication and signaling : CCS · 2026Review
- ATR and PKMYT1 Inhibition Resensitizes a Subset of TNBC Patient-Derived Models to Carboplatin, Inducing Mitotic Catastrophe.Cancer research communications · 2026Article
- Advances in BRET probes for intracellular target engagement studies.Nature chemical biology · 2026Review
- Glioblastoma invasion into different organoid hosts reveals cell-intrinsic and proliferative migratory programs.iScience · 2026Article
- CRISPR screening redefines therapeutic target identification and drug discovery with precision and scalability.Journal of pharmaceutical analysis · 2026Review
- Targeting PKMYT1 enhances antitumor immune responses to PD-L1 blockade in castration-resistant prostate cancer.Journal for immunotherapy of cancer · 2026Article
- Real-world data on the clinical impact of molecular tumor boards in high- and low-grade serous ovarian cancer.Frontiers in oncology · 2026Article
- E2F1-mediated PKMYT1 upregulation promotes prostate cancer progression by inhibiting the PPAR signaling pathway.Scientific reports · 2025Article
- Discovery of a bifunctional PKMYT1-targeting PROTAC empowered by AI-generation.Nature communications · 2025Article
- WEE1 inhibitors trigger GCN2-mediated activation of the integrated stress response.Nature communications · 2025Article
- Genome instability and crosstalk with the immune response.Genome medicine · 2025Review
- WEE1 inhibitors synergise with mRNA translation defects via activation of the kinase GCN2.Nature communications · 2025Article
- Exploring PKMYT1 as a potential marker for colorectal cancer progression through bioinformatics analyses and experimental validation.Scientific reports · 2025Article
- Integrated multi-omics analysis identifies SELENOP and PKMYT1 as immune-metabolic hub genes in breast cancer.Biochemistry and biophysics reports · 2025Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
31 authors at 4 institutions in 2 countries.
Janek SzychowskiRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.ORCID 0000-0002-0630-9856
Robert PappRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Evelyne DietrichRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Bingcan LiuRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Frédéric ValléeRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Marie-Eve LeclaireRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Jimmy FourtounisRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Giovanni MartinoRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Alexander L PerrymanRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Victor PauLunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.ORCID 0000-0002-3093-2330
Shou Yun YinRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Pavel MaderLunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.ORCID 0000-0002-0820-2761
Anne RoulstonRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Jean-Francois TruchonRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
C Gary MarshallRepare Therapeutics, 1 Broadway, 15th Floor, Cambridge, Massachusetts 02142, United States.
Mohamed DialloRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Nicole M DuffyRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Rino StoccoRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Claude GodboutRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Alexanne Bonneau-FortinRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Rosie KryczkaRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Vivek BhaskaranRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Daniel MaoLunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.
Stephen OrlickyLunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.
Patrick BeaulieuOmegaChem Inc., 480 Rue Perreault, Saint-Romuald, QC G6W 7V6, Canada.
Pascal TurcotteAdMare BioInnovations, 7171 Frederick-Banting, Montréal, QC H4S 1Z9, Canada.
Igor KurinovDepartment of Chemistry and Chemical Biology, Cornell University, NE-CAT, Argonne, Illinois 60439, United States.
Frank SicheriLunenfeld-Tanenbaum Research Institute, Sinai Health System, Toronto, ON M5G 1X5, Canada.ORCID 0000-0002-9824-2117
Yael MamaneRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Michel GallantRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
W Cameron BlackRepare Therapeutics, Inc., 7210 Frederick-Banting, Ville St-Laurent, QC H4S 2A1, Canada.
Lunenfeld-Tanenbaum Research Institute · CAArgonne National Laboratory · USOmegaChem (Canada) · CAUniversity of Toronto · CA
Funding
User Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI MALCOLM S. CAPEL · 2018 to 2026
$34.2MCIHRNIGMS NIH HHS P30 GM124165
Abstract
PKMYT1 is a regulator of CDK1 phosphorylation and is a compelling therapeutic target for the treatment of certain types of DNA damage response cancers due to its established synthetic lethal relationship with
Indexed as
NeoplasmsProtein-Tyrosine KinasesCell Line, TumorCell ProliferationHumansMembrane ProteinsProtein Kinase InhibitorsProtein Serine-Threonine KinasesMembrane ProteinsPKMYT1 protein, humanProtein Kinase InhibitorsProtein Serine-Threonine KinasesProtein-Tyrosine Kinases
Identifiers
What OpenQuestion holds
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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.