Unknown,Transcriptomics,Genomics,Proteomics

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P493-6 treated with KJ-Pyr-9 and/or Doxycycline

ABSTRACT: In a fluorescence polarization screen for 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-overexpressing  human cancer cells. 4 treatment groups analyzed in triplicate: no treatment(control), 20uM KJ-Pyr-9, 0.1ug/mL doxycycline and KJ-Pyr-9 in combination with doxycycline

ORGANISM(S): Homo sapiens

SUBMITTER: Jonathan Hart 

PROVIDER: E-GEOD-58168 | biostudies-arrayexpress |

REPOSITORIES: biostudies-arrayexpress

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Inhibitor of MYC identified in a Kröhnke pyridine library.

Hart Jonathan R JR   Garner Amanda L AL   Yu Jing J   Ito Yoshihiro Y   Sun Minghao M   Ueno Lynn L   Rhee Jin-Kyu JK   Baksh Michael M MM   Stefan Eduard E   Hartl Markus M   Bister Klaus K   Vogt Peter K PK   Janda Kim D KD  

Proceedings of the National Academy of Sciences of the United States of America 20140811 34

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 wea  ...[more]

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