6HK6

Human RIOK2 bound to inhibitor

6HK6 の概要

• エントリーDOI: 10.2210/pdb6hk6/pdb
• 分子名称: Serine/threonine-protein kinase RIO2, 2-naphthalen-2-yl-~{N}-pyridin-2-yl-ethanamide, CHLORIDE ION, ... (6 entities in total)
• 機能のキーワード: kinase, structural genomics consortium, sgc, transferase
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 10
• 化学式量合計: 386800.42

構造登録者

Wang, J.,Krojer, T.,Bountra, C.,Edwards, A.M.,Arrowsmith, C.,Knapp, S.,Elkins, J.M. (登録日: 2018-09-05, 公開日: 2018-10-24, 最終更新日: 2024-01-17)

主引用文献

Wang, J.,Varin, T.,Vieth, M.,Elkins, J.M.
Crystal structure of human RIOK2 bound to a specific inhibitor.
Open Biology, 9:190037-190037, 2019

PubMed Abstract: The RIO kinases (RIOKs) are a universal family of atypical kinases that are essential for assembly of the pre-40S ribosome complex. Here, we present the crystal structure of human RIO kinase 2 (RIOK2) bound to a specific inhibitor. This first crystal structure of an inhibitor-bound RIO kinase reveals the binding mode of the inhibitor and explains the structure-activity relationship of the inhibitor series. The inhibitor binds in the ATP-binding site and forms extensive hydrophobic interactions with residues at the entrance to the ATP-binding site. Analysis of the conservation of active site residues reveals the reasons for the specificity of the inhibitor for RIOK2 over RIOK1 and RIOK3, and it provides a template for inhibitor design against the human RIOK family.

PubMed: 30991936
DOI: 10.1098/rsob.190037

実験手法

X-RAY DIFFRACTION (2.35 Å)