Inhibitor of MYC identified in a Kröhnke pyridine library

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 K d of KJ-Pyr-9 for MYC in vitro is 6.5 ± 1.0 nM, as determined by backscattering interferometry; KJ-Pyr-9 also interferes wit...

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Published in:	Proceedings of the National Academy of Sciences - PNAS 2014-08, Vol.111 (34), p.12556-12561
Main Authors:	Hart, Jonathan R., Garner, Amanda L., Yu, Jing, Ito, Yoshihiro, Sun, Minghao, Ueno, Lynn, Rhee, Jin-Kyu, Baksh, Michael M., Stefan, Eduard, Hartl, Markus, Bister, Klaus, Vogt, Peter K., Janda, Kim D.
Format:	Article
Language:	English
Subjects:	Animals Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Basic Helix-Loop-Helix Leucine Zipper Transcription Factors - antagonists & inhibitors Basic Helix-Loop-Helix Leucine Zipper Transcription Factors - chemistry Biological Sciences birds Cancer cell culture Cell culture techniques Cell growth Cell lines Cell Proliferation - drug effects Cell Transformation, Neoplastic - drug effects Cell Transformation, Neoplastic - genetics Cells, Cultured Chick Embryo Drug Evaluation, Preclinical Female Fibroblasts Fluorescence Fluorescence Polarization Genes Genes, myc Humans Inhibitor drugs Interferometry Mice Mice, Nude Molecules Multiprotein Complexes - antagonists & inhibitors Multiprotein Complexes - chemistry neoplasm cells neoplasms oncogene proteins Oncology Protein Interaction Domains and Motifs - drug effects Proteins Proto-Oncogene Proteins c-myc - antagonists & inhibitors Proto-Oncogene Proteins c-myc - chemistry pyridines Pyridines - chemistry Pyridines - pharmacology Pyrimidines - chemistry Pyrimidines - pharmacology Signatures transcription (genetics) Tumors Xenograft Model Antitumor Assays
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