Development of Allosteric NIK Ligands from Fragment-Based NMR Screening.
ACS Med Chem Lett
; 14(12): 1815-1820, 2023 Dec 14.
Article
em En
| MEDLINE
| ID: mdl-38116406
ABSTRACT
NF-κB inducing kinase (NIK) is vital for the induction of many immune responses, and as such, NIK dysregulation has been implicated in various inflammatory diseases and cancers. NIK has been pursued as a potential therapeutic target, and small-molecule inhibitors that bind the orthosteric site on NIK have been reported. However, despite the established chemical matter, NIK inhibitors have not yet reached the clinic. With the goal of developing allosteric NIK ligands using a fragment-based NMR screening approach, we report the identification and development of a series of allosteric, fragment-sized NIK ligands that bind with micromolar potency and good ligand efficiency.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Idioma:
En
Revista:
ACS Med Chem Lett
Ano de publicação:
2023
Tipo de documento:
Article
País de afiliação:
Estados Unidos