3UZP

crystal structure of ck1d with PF670462 from P21 crystal form

3UZP の概要

• エントリーDOI: 10.2210/pdb3uzp/pdb
• 関連するPDBエントリー: 1CKI 3UYS 3UYT
• 分子名称: Casein kinase I isoform delta, 4-[1-cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]pyrimidin-2-amine (3 entities in total)
• 機能のキーワード: ck1d, kinase, inhibitor, pf670462, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm: P48730
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 69376.11

構造登録者

Huang, X. (登録日: 2011-12-07, 公開日: 2012-01-11, 最終更新日: 2024-02-28)

主引用文献

Long, A.,Zhao, H.,Huang, X.
Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.
J.Med.Chem., 55:956-960, 2012

PubMed Abstract: Casein kinase 1 delta (CK1δ) and its closest homologue CK1ε are key regulators of diverse cellular growth and survival processes such as Wnt signaling, DNA repair, and circadian rhythms. We report three crystal structures of the kinase domain of human CK1δ, one apo and two complexed with a potent and selective CK1δ/ε inhibitor PF670462 in two different crystal forms. These structures provide a molecular basis for the strong and specific inhibitor interactions and suggest clues for further development of CK1δ/ε inhibitors.

PubMed: 22168824
DOI: 10.1021/jm201387s

実験手法

X-RAY DIFFRACTION (1.94 Å)