Title of article
Discovery of novel and selective IKK-β serine-threonine protein kinase inhibitors. Part 1
Author/Authors
Toshiki Murata، نويسنده , , Mitsuyuki Shimada، نويسنده , , Sachiko Sakakibara، نويسنده , , Takashi Yoshino ، نويسنده , , Hiroshi Kadono، نويسنده , , Tsutomu Masuda، نويسنده , , Makoto Shimazaki، نويسنده , , Takuya Shintani، نويسنده , , Kinji Fuchikami، نويسنده , , Katsuya Sakai، نويسنده , , Hisayo Inbe، نويسنده , , Keisuke Takeshita، نويسنده , , Toshiro Niki، نويسنده , , Masaomi Umeda، نويسنده , , Kevin B. Bacon، نويسنده , , Karl B. Ziegelbauer، نويسنده , , Timothy B. Lowinger، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
6
From page
913
To page
918
Abstract
IκB kinase β (IKK-β) is a serine-threonine protein kinase critically involved in the activation of the transcription factor Nuclear Factor kappa B (NF-κB) in response to various inflammatory stimuli. We have identified a small molecule inhibitor of IKK-β. Optimization of the lead compound resulted in improvements in both in vitro and in vivo potency, and provided IKK-β inhibitors exhibiting potent activity in an acute cytokine release model (LPS-induced TNFα).
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793044
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