Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity

The chromatin-associated protein WDR5 is a promising target for pharmacological inhibition in cancer. Drug discovery efforts center on the blockade of the “WIN site” of WDR5, a well-defined pocket that is amenable to small molecule inhibition. Various cancer contexts have been proposed to be targets...

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Bibliografiska uppgifter
I publikationen:Cell Rep
Huvudupphovsmän: Aho, Erin R., Wang, Jing, Gogliotti, Rocco D., Howard, Gregory C., Phan, Jason, Acharya, Pankaj, Macdonald, Jonathan D., Cheng, Ken, Lorey, Shelly L., Lu, Bin, Wenzel, Sabine, Foshage, Audra M., Alvarado, Joseph, Wang, Feng, Shaw, J. Grace, Zhao, Bin, Weissmiller, April M., Thomas, Lance R., Vakoc, Christopher R., Hall, Matthew D., Hiebert, Scott W., Liu, Qi, Stauffer, Shaun R., Fesik, Stephen W., Tansey, William P.
Materialtyp: Artigo
Språk:Inglês
Publicerad: 2019
Ämnen:
Article
Länkar:https://ncbi.nlm.nih.gov/pmc/articles/PMC6448596/
https://ncbi.nlm.nih.gov/pubmed/30865883
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.celrep.2019.02.047
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