Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability

Pharmacological activation of NRF2 (Nuclear factor erythroid 2-related factor 2) arises from blocking interaction of NRF2 with its negative regulator, KEAP1 (Kelch-like ECH-associated protein 1). We previously reported an isoquinoline-based NRF2 activator, but this compound showed negative logD(7.4)...

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Pubblicato in:J Med Chem
Autori principali: Lazzara, Phillip R., David, Brian P., Ankireddy, Aparna, Richardson, Benjamin G., Dye, Katherine, Ratia, Kiira M., Reddy, Sekhar P., Moore, Terry W.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2019
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC7315935/
https://ncbi.nlm.nih.gov/pubmed/31682434
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b01074
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