6JWA

Crystal structure of CK2a1 with 5-iodotubercidin

6JWA の概要

• エントリーDOI: 10.2210/pdb6jwa/pdb
• 分子名称: Casein kinase II subunit alpha, (2R,3R,4S,5R)-2-(4-AMINO-5-IODO-7H-PYRROLO[2,3-D]PYRIMIDIN-7-YL)-5-(HYDROXYMETHYL)TETRAHYDROFURAN-3,4-DIOL, 1,2-ETHANEDIOL, ... (4 entities in total)
• 機能のキーワード: protein kinase, transferase, inhibitor, complex
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 41242.75

構造登録者

Tsuyuguchi, M.,Kinoshita, T. (登録日: 2019-04-19, 公開日: 2019-07-24, 最終更新日: 2023-11-22)

主引用文献

Tsuyuguchi, M.,Nakaniwa, T.,Sawa, M.,Nakanishi, I.,Kinoshita, T.
A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1.
Acta Crystallogr.,Sect.F, 75:515-519, 2019

PubMed Abstract: Protein kinase CK2a1 is a serine/threonine kinase that plays a crucial role in the growth, proliferation and survival of cells and is a well known target for tumour and glomerulonephritis therapies. Here, the crystal structure of the kinase domain of CK2a1 complexed with 5-iodotubercidin (5IOD), an ATP-mimetic inhibitor, was determined at 1.78 Å resolution. The structure shows distinct structural features and, in combination with a comparison of the crystal structures of five off-target kinases complexed with 5IOD, provides valuable information for the development of highly selective inhibitors.

PubMed: 31282872
DOI: 10.1107/S2053230X19008951

実験手法

X-RAY DIFFRACTION (1.781 Å)