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Discovery of novel and selective IKK-beta serine-threonine protein kinase inhibitors. Part 1.

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).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

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

doi

10.1016/s0960-894x(02)01046-6

subject

Has Abstract

pub_date

2003-03-10 00:00:00

pages

913-8

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960894X02010466

journal_volume

13

pub_type

杂志文章

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