4HOK

crystal structure of apo ck1e

4HOK の概要

• エントリーDOI: 10.2210/pdb4hok/pdb
• 関連するPDBエントリー: 4HNF 4HNI
• 分子名称: Casein kinase I isoform epsilon, SULFATE ION (3 entities in total)
• 機能のキーワード: ck1e, kinase, inhibitor, pf 4800567, transferase
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 12
• 化学式量合計: 412940.11

構造登録者

Huang, X.,Long, A.M.,Zhao, H. (登録日: 2012-10-22, 公開日: 2012-11-14, 最終更新日: 2024-02-28)

主引用文献

Long, A.M.,Zhao, H.,Huang, X.
Structural basis for the potent and selective inhibition of casein kinase 1 epsilon.
J.Med.Chem., 55:10307-10311, 2012

PubMed Abstract: Casein kinase 1 epsilon (CK1ε) and its closest homologue CK1δ are key regulators of diverse cellular processes. We report two crystal structures of PF4800567, a potent and selective inhibitor of CK1ε, bound to the kinase domains of human CK1ε and CK1δ as well as one apo CK1ε crystal structure. These structures provide a molecular basis for the strong and specific inhibitor interactions with CK1ε and suggest clues for further development of CK1δ inhibitors.

PubMed: 23106386
DOI: 10.1021/jm301336n

実験手法

X-RAY DIFFRACTION (2.77 Å)