Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation

[Image: see text] We describe the discovery of three structurally differentiated potent and selective MTH1 inhibitors and their subsequent use to investigate MTH1 as an oncology target, culminating in target (in)validation. Tetrahydronaphthyridine 5 was rapidly identified as a highly potent MTH1 inh...

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Pubblicato in:ACS Med Chem Lett
Autori principali: Farand, Julie, Kropf, Jeffrey E., Blomgren, Peter, Xu, Jianjun, Schmitt, Aaron C., Newby, Zachary E., Wang, Ting, Murakami, Eisuke, Barauskas, Ona, Sudhamsu, Jawahar, Feng, Joy Y., Niedziela-Majka, Anita, Schultz, Brian E., Schwartz, Karen, Viatchenko-Karpinski, Serge, Kornyeyev, Dmytro, Kashishian, Adam, Fan, Peidong, Chen, Xiaowu, Lansdon, Eric B., Ports, Michael O., Currie, Kevin S., Watkins, William J., Notte, Gregory T.
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2019
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC7074220/
https://ncbi.nlm.nih.gov/pubmed/32184970
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00420
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