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Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91

Napabucasin, undergoing multiple clinical trials, was reported to inhibit the signal transducer and transcription factor 3 (STAT3). To better elucidate its mechanism of action, we designed a napabucasin-based proteolysis targeting chimera (PROTAC), XD2–149 that resulted in inhibition of STAT3 signal...

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Pubblicato in:J Med Chem
Autori principali: Hanafi, Maha, Chen, Xinde, Neamati, Nouri
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2021
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC8083113/
https://ncbi.nlm.nih.gov/pubmed/33506674
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c01897
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