Structure-Guided DOT1L Probe Optimization by Label-Free Ligand Displacement

[Image: see text] The DOT1L lysine methyltransferase has emerged as a validated therapeutic target in MLL-rearranged (MLLr) acute leukemias. Although S-adenosylmethionine competitive inhibitors have demonstrated pharmacological proof-of-principle in MLLr-leukemia, these compounds require further opt...

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Publicat a:ACS Chem Biol
Autors principals: Yi, Joanna S., Federation, Alexander J., Qi, Jun, Dhe-Paganon, Sirano, Hadler, Michael, Xu, Xiang, St. Pierre, Roodolph, Varca, Anthony C., Wu, Lei, Marineau, Jason J., Smith, William B., Souza, Amanda, Chory, Emma J., Armstrong, Scott A., Bradner, James E.
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2014
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC4504433/
https://ncbi.nlm.nih.gov/pubmed/25397901
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/cb500796d
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