ArticleProceedings of the National Academy of Sciences of the United States of America2014
Inhibitor of MYC identified in a Kröhnke pyridine library.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 91 papers.
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Who cites it
91 citing papers in PubMed, 143 citations in OpenAlex.
- Cancer Genes: Origins and Directions.Viruses · 2026Review
- Insights into the Design of MYC-Targeting Proteolysis Targeting Chimeras (PROTACs).Molecules (Basel, Switzerland) · 2026Article
- Reactivation of the silencedProceedings of the National Academy of Sciences of the United States of America · 2026Article
- Probing the Structural Dynamics of the Unbound MAX Protein: Insights from Well-Tempered Metadynamics.Journal of chemical information and modeling · 2026Article
- Solid-phase synthesis of a pyrrole library and identification of bioactive compounds.Bioorganic & medicinal chemistry letters · 2025Article
- Pan-cancer Myc modulator that targets Myc-α-tubulin interaction to drive selective mitotic catastrophe.Scientific reports · 2025Article
- Targeting MYC: Multidimensional regulation and therapeutic strategies in oncology.Genes & diseases · 2025Review
- Beyond the Limit: MYC Mediates Tumor Immune Escape.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Recent Advances in Pineoblastoma Research: Molecular Classification, Modelling and Targetable Vulnerabilities.Cancers · 2025Review
- The Effect of Myc Inhibition Combined with the Synergistic Effect of Photothermal, Photodynamic and Radiotherapy in Tumor Treatment.International journal of nanomedicine · 2025Review
- New Insights into Potential Therapeutic Targets for Neuroendocrine Prostate Cancer: From Bench to Clinic.Research (Washington, D.C.) · 2025Review
- Latest Therapeutical Approaches for Triple-Negative Breast Cancer: From Preclinical to Clinical Research.International journal of molecular sciences · 2024Review
- Targeting TNF/IL-17/MAPK pathway in hHaematologica · 2024Article
- ELP3 stabilizes c-Myc to promote tumorigenesis.Journal of molecular cell biology · 2024Article
- MYC activity at enhancers drives prognostic transcriptional programs through an epigenetic switch.Nature genetics · 2024Article
- Myeloid-Mas Signaling Modulates Pathogenic Crosstalk among MYCAdvanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Antitumor efficacy of a sequence-specific DNA-targeted γPNA-based c-Myc inhibitor.Cell reports. Medicine · 2024Article
- Nilotinib: Disrupting the MYC-MAX Heterocomplex.Bioinformatics and biology insights · 2024Article
- IL-15 Priming Alters IFN-γ Regulation in Murine NK Cells.Journal of immunology (Baltimore, Md. : 1950) · 2023Article
- MYC is a clinically significant driver of mTOR inhibitor resistance in breast cancer.The Journal of experimental medicine · 2023Article
31 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 2 countries.
Funding
Abstract
In a fluorescence polarization screen for the MYC-MAX interaction, we have identified a novel small-molecule inhibitor of MYC, KJ-Pyr-9, from a Kröhnke pyridine library. The Kd of KJ-Pyr-9 for MYC in vitro is 6.5 ± 1.0 nM, as determined by backscattering interferometry; KJ-Pyr-9 also interferes with MYC-MAX complex formation in the cell, as shown in a protein fragment complementation assay. KJ-Pyr-9 specifically inhibits MYC-induced oncogenic transformation in cell culture; it has no or only weak effects on the oncogenic activity of several unrelated oncoproteins. KJ-Pyr-9 preferentially interferes with the proliferation of MYC-overexpressing human and avian cells and specifically reduces the MYC-driven transcriptional signature. In vivo, KJ-Pyr-9 effectively blocks the growth of a xenotransplant of MYC-amplified human cancer cells.
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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.