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ID: ALA1136626
Journal: Bioorg Med Chem Lett
Title: Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1.
Authors: Murata T, Shimada M, Sakakibara S, Yoshino T, Kadono H, Masuda T, Shimazaki M, Shintani T, Fuchikami K, Sakai K, Inbe H, Takeshita K, Niki T, Umeda M, Bacon KB, Ziegelbauer KB, Lowinger TB.
Abstract: IkappaB kinase beta (IKK-beta) is a serine-threonine protein kinase critically involved in the activation of the transcription factor Nuclear Factor kappa B (NF-kappaB) in response to various inflammatory stimuli. We have identified a small molecule inhibitor of IKK-beta. Optimization of the lead compound resulted in improvements in both in vitro and in vivo potency, and provided IKK-beta inhibitors exhibiting potent activity in an acute cytokine release model (LPS-induced TNFalpha).
CiteXplore: 12617920