Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

The addressable pocket of a protein is often not functionally relevant in disease. This is true for the multidomain, bromodomain-containing transcriptional regulator TRIM24. TRIM24 has been posited as a dependency in numerous cancers, yet potent and selective ligands for the TRIM24 bromodomain do no...

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Publicado en:Nat Chem Biol
Autores principales: Gechijian, Lara N., Buckley, Dennis L., Lawlor, Matthew A., Reyes, Jaime M., Paulk, Joshiawa, Ott, Christopher J., Winter, Georg E., Erb, Michael A., Scott, Thomas G., Xu, Mousheng, Seo, Hyuk-Soo, Dhe-Paganon, Sirano, Kwiatkowski, Nicholas P., Perry, Jennifer A., Qi, Jun, Gray, Nathanael S., Bradner, James E.
Formato: Artigo
Lenguaje:Inglês
Publicado: 2018
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Article
Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC5866761/
https://ncbi.nlm.nih.gov/pubmed/29507391
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41589-018-0010-y
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