1A9U

THE COMPLEX STRUCTURE OF THE MAP KINASE P38/SB203580

1A9U の概要

• エントリーDOI: 10.2210/pdb1a9u/pdb
• 分子名称: MAP KINASE P38, 4-[5-(4-FLUORO-PHENYL)-2-(4-METHANESULFINYL-PHENYL)-3H-IMIDAZOL-4-YL]-PYRIDINE (3 entities in total)
• 機能のキーワード: transferase, map kinase, serine/threonine-protein kinase, p38
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm : Q16539
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 43760.79

構造登録者

Wang, Z.,Canagarajah, B.,Boehm, J.C.,Kassis, S.,Cobb, M.H.,Young, P.R.,Abdel-Meguid, S.,Adams, J.L.,Goldsmith, E.J. (登録日: 1998-04-10, 公開日: 1999-04-20, 最終更新日: 2024-04-03)

主引用文献

Wang, Z.,Canagarajah, B.J.,Boehm, J.C.,Kassisa, S.,Cobb, M.H.,Young, P.R.,Abdel-Meguid, S.,Adams, J.L.,Goldsmith, E.J.
Structural basis of inhibitor selectivity in MAP kinases.
Structure, 6:1117-1128, 1998

PubMed Abstract: The mitogen-activated protein (MAP) kinases are important signaling molecules that participate in diverse cellular events and are potential targets for intervention in inflammation, cancer, and other diseases. The MAP kinase p38 is responsive to environmental stresses and is involved in the production of cytokines during inflammation. In contrast, the activation of the MAP kinase ERK2 (extracellular-signal-regulated kinase 2) leads to cellular differentiation or proliferation. The anti-inflammatory agent pyridinylimidazole and its analogs (SB [SmithKline Beecham] compounds) are highly potent and selective inhibitors of p38, but not of the closely-related ERK2, or other serine/threonine kinases. Although these compounds are known to bind to the ATP-binding site, the origin of the inhibitory specificity toward p38 is not clear.

PubMed: 9753691
DOI: 10.1016/S0969-2126(98)00113-0

実験手法

X-RAY DIFFRACTION (2.5 Å)