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Updated: Oct 21, 2025

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
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CBP/p300のダブルサイト阻害剤KIXは,Mybの選択的かつ効果的な調節剤である

Stephen T Joy1, Madeleine J Henley1,2, Samantha N De Salle1,2

  • 1Life Sciences Institute, University of Michigan, Ann Arbor, Michigan 48109, United States.

Journal of the American Chemical Society
|September 7, 2021
PubMed
まとめ

研究者はMybLL-tideを開発し,急性骨髄性白血病 (AML) および他の癌において重要なMyb- CBP/ p300 KIX相互作用を標的とした強力な二重サイト阻害剤を開発した.

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Transcriptional regulators bind to specific cis-regulatory sequences in the DNA to regulate gene transcription. These cis-regulatory sequences are very short, usually less than ten nucleotide pairs in length. The short length means that there is a high probability of the exact same sequence randomly occurring throughout the genome.  Since regulators can also bind to groups of similar sequences, this further increases the chances of random binding. Transcriptional regulators form...
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