Details

Autor(en) / Beteiligte

• Pippione, Agnese C
• Sainas, Stefano
• Federico, Antonella
• Lupino, Elisa
• Piccinini, Marco
• Kubbutat, Michael
• Contreras, Jean-Marie
• Morice, Christophe
• Barge, Alessandro
• Ducime, Alex
• Boschi, Donatella
• Al-Karadaghi, Salam
• Lolli, Marco L

Titel

N -Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK

Ist Teil von

• MedChemComm, 2018, Vol.9 (6), p.963-968

Ort / Verlag

England: Royal Society of Chemistry

Erscheinungsjahr

2018

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• NF-κB-inducing kinase (NIK), an oncogenic drug target that is associated with various cancers, is a central signalling component of the non-canonical pathway. A blind screening process, which established that amino pyrazole related scaffolds have an effect on IKKbeta, led to a optimization process that identified the aminopyrazole as a low μM selective NIK inhibitor. Compound effectively inhibited the NIK-dependent activation of the NF-κB pathway in tumour cells, confirming its selective inhibitory profile.