High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2

The histone lysine methyltransferase nuclear receptor-binding SET domain protein 2 (NSD2, also known as WHSC1/MMSET) is an epigenetic modifier and is thought to play a driving role in oncogenesis. Both NSD2 overexpression and point mutations that increase its catalytic activity are associated with s...

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Pubblicato in:J Biol Chem
Autori principali: Coussens, Nathan P., Kales, Stephen C., Henderson, Mark J., Lee, Olivia W., Horiuchi, Kurumi Y., Wang, Yuren, Chen, Qing, Kuznetsova, Ekaterina, Wu, Jianghong, Chakka, Sirisha, Cheff, Dorian M., Cheng, Ken Chih-Chien, Shinn, Paul, Brimacombe, Kyle R., Shen, Min, Simeonov, Anton, Lal-Nag, Madhu, Ma, Haiching, Jadhav, Ajit, Hall, Matthew D.
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Society for Biochemistry and Molecular Biology 2018
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC6120216/
https://ncbi.nlm.nih.gov/pubmed/29945974
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/jbc.RA118.004274
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