4RSS

Crystal structure of tyrosine-protein kinase SYK with an inhibitor

4RSS の概要

• エントリーDOI: 10.2210/pdb4rss/pdb
• 分子名称: Tyrosine-protein kinase SYK, 1-[(3-methyl-1-{2-[(1,2,3-trimethyl-1H-indol-5-yl)amino]pyrimidin-4-yl}-1H-pyrazol-4-yl)methyl]azetidin-3-ol (3 entities in total)
• 機能のキーワード: kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cell membrane : P43405
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 34318.47

構造登録者

Lee, B.I.,Lee, S.J.,Choi, J.-S. (登録日: 2014-11-11, 公開日: 2015-10-21, 最終更新日: 2024-03-20)

主引用文献

Choi, J.S.,Hwang, H.J.,Kim, S.W.,Lee, B.I.,Lee, J.,Song, H.J.,Koh, J.S.,Kim, J.H.,Lee, P.H.
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.
Bioorg.Med.Chem.Lett., 25:4441-4446, 2015

PubMed Abstract: A series of pyrazolylpyrimidine scaffold based Syk inhibitors were synthesized and evaluated for their biological activities and selectivity. Lead optimization efforts provided compounds with potent Syk inhibition in both enzymatic and TNF-α release assay.

PubMed: 26384287
DOI: 10.1016/j.bmcl.2015.09.011

実験手法

X-RAY DIFFRACTION (1.83 Å)