Structure Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase

Selective inhibitors of protein lysine methyltransferases, including SET domain-containing protein 8 (SETD8), are highly desired, as only a fraction of these enzymes are associated with high-quality inhibitors. From our previously discovered SETD8 inhibitor, we developed a more potent analog and sol...

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Veröffentlicht in:J Med Chem
Hauptverfasser: Butler, Kyle V., Ma, Anqi, Yu, Wenyu, Li, Fengling, Tempel, Wolfram, Babault, Nicolas, Pittella-Silva, Fabio, Shao, Jason, Wang, Junyi, Luo, Minkui, Vedadi, Masoud, Brown, Peter J., Arrowsmith, Cheryl H., Jin, Jian
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2016
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5148670/
https://ncbi.nlm.nih.gov/pubmed/27804297
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01244
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