NF-κB-inducing kinase (NIK) is a protein kinase central to the noncanonical NF-κB pathway downstream from multiple TNF receptor family members, including BAFF, which has been associated with B cell survival and maturation, dendritic cell activation, secondary lymphoid organ development, and bone metabolism. We report herein the discovery of lead chemical series of NIK inhibitors that were identified through a scaffold-hopping strategy using structure-based design. Electronic and steric properties of lead compounds were modified to address glutathione conjugation and amide hydrolysis. These highly potent compounds exhibited selective inhibition of LTβR-dependent p52 translocation and transcription of NF-κB2 related genes. Compound <b>4f</b> ...
Transcription factors of the nuclear factor κB (NF-κB) family are central coordinating regulators of...
Recent studies suggest that nuclear factor κB-inducing kinase (NIK) is suppressed through constituti...
Despite the impressive accomplishments in the development of small molecule kinase inhibitors over t...
NF-κB-inducing kinase (NIK) is a protein kinase central to the noncanonical NF-κB pathway downstream...
We report here structure-guided optimization of a novel series of NF-κB inducing kinase (NIK) inhibi...
SummaryThe NF-κB inducing kinase (NIK) regulates the non-canonical NF-κB pathway downstream of impor...
As a wide variety of pro-inflammatory cytokines are involved in the development of rheumatoid arthri...
NF-κB-inducing kinase (NIK) is a key player in non-canonical NF-κB signaling, involved in several fu...
Excessive NF-κB activation contributes to the pathogenesis of numerous diseases. Small-molecule inhi...
In this issue of Structure, de Leon-Boenig and colleagues bring to light several key characteristics...
ATP competitive compounds have been synthesised which exhibit single digit micromolar potency agains...
As a wide variety of pro-inflammatory cytokines are involved in the development of rheumatoid arthri...
Previously held under moratorium from 12th March 2018 until 7th June 2023.The dysregulation of the t...
The cellular kinases inhibitory-κB kinase (IKK) α and Nuclear Factor-κB (NF-&kappa...
Transcription factors of the NF-κB family are driven by many inflammatory stimuli and activate expre...
Transcription factors of the nuclear factor κB (NF-κB) family are central coordinating regulators of...
Recent studies suggest that nuclear factor κB-inducing kinase (NIK) is suppressed through constituti...
Despite the impressive accomplishments in the development of small molecule kinase inhibitors over t...
NF-κB-inducing kinase (NIK) is a protein kinase central to the noncanonical NF-κB pathway downstream...
We report here structure-guided optimization of a novel series of NF-κB inducing kinase (NIK) inhibi...
SummaryThe NF-κB inducing kinase (NIK) regulates the non-canonical NF-κB pathway downstream of impor...
As a wide variety of pro-inflammatory cytokines are involved in the development of rheumatoid arthri...
NF-κB-inducing kinase (NIK) is a key player in non-canonical NF-κB signaling, involved in several fu...
Excessive NF-κB activation contributes to the pathogenesis of numerous diseases. Small-molecule inhi...
In this issue of Structure, de Leon-Boenig and colleagues bring to light several key characteristics...
ATP competitive compounds have been synthesised which exhibit single digit micromolar potency agains...
As a wide variety of pro-inflammatory cytokines are involved in the development of rheumatoid arthri...
Previously held under moratorium from 12th March 2018 until 7th June 2023.The dysregulation of the t...
The cellular kinases inhibitory-κB kinase (IKK) α and Nuclear Factor-κB (NF-&kappa...
Transcription factors of the NF-κB family are driven by many inflammatory stimuli and activate expre...
Transcription factors of the nuclear factor κB (NF-κB) family are central coordinating regulators of...
Recent studies suggest that nuclear factor κB-inducing kinase (NIK) is suppressed through constituti...
Despite the impressive accomplishments in the development of small molecule kinase inhibitors over t...