Covalent Inhibitors of KEAP1 with Exquisite Selectivity

The NRF2-KEAP1 interaction is central for cytoprotection against stresses, giving it high clinical significance. Covalent modification of KEAP1 is an efficient approach, but the covalent inhibitors used in the clinic carry undesired side effects originating in their moderate selectivity. Starting wi...

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Veröffentlicht in:	Journal of medicinal chemistry 2024-12, Vol.67 (23), p.21208-21222
Hauptverfasser:	Fejes, Imre, Markacz, Piroska, Tatai, Janos, Rudas, Monika, Dunkel, Petra, Gyuris, Mario, Nyerges, Miklos, Provost, Nicolas, Duvivier, Valérie, Delerive, Philippe, Martiny, Virginie, Bristiel, Alexandra, Vidal, Brice, Richardson, William, Rothweiler, Elisabeth M., Tranberg-Jensen, Jeppe, Manning, Charlotte E., Sweeney, Melissa N., Chalk, Rod, Huber, Kilian V. M., Bullock, Alex N., Herner, Andras, Seedorf, Klaus, Vinson, Cedric, Weber, Csaba, Kotschy, Andras
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Crystallography, X-Ray Humans Kelch-Like ECH-Associated Protein 1 - antagonists & inhibitors Kelch-Like ECH-Associated Protein 1 - metabolism Mice Models, Molecular NF-E2-Related Factor 2 - antagonists & inhibitors NF-E2-Related Factor 2 - metabolism Structure-Activity Relationship
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