6GVJ

Human Mps1 kinase domain with ordered activation loop

6GVJ の概要

• エントリーDOI: 10.2210/pdb6gvj/pdb
• 分子名称: Dual specificity protein kinase TTK, GLYCEROL, CHLORIDE ION, ... (4 entities in total)
• 機能のキーワード: mps1, ttk, kinase, mitosis checkpoint, transferase, activation loop, activation segment
• 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: 49496.04

構造登録者

Roorda, J.C.,Hiruma, Y.,Joosten, R.P.,Perrakis, A. (登録日: 2018-06-21, 公開日: 2019-01-09, 最終更新日: 2024-01-17)

主引用文献

Roorda, J.C.,Joosten, R.P.,Perrakis, A.,Hiruma, Y.
A crystal structure of the human protein kinase Mps1 reveals an ordered conformation of the activation loop.
Proteins, 87:348-352, 2019

PubMed Abstract: Monopolar spindle 1 (Mps1) is a dual-specificity protein kinase, orchestrating faithful chromosome segregation during mitosis. All reported structures of the Mps1 kinase adopt the hallmarks of an inactive conformation, which includes a mostly disordered activation loop. Here, we present a 2.4 Å resolution crystal structure of an "extended" version of the Mps1 kinase domain, which shows an ordered activation loop. However, the other structural characteristics of an active kinase are not present. Our structure shows that the Mps1 activation loop can fit to the ATP binding pocket and interferes with ATP, but less so with inhibitors binding, partly explain the potency of various Mps1 inhibitors.

PubMed: 30582207
DOI: 10.1002/prot.25651

実験手法

X-RAY DIFFRACTION (2.41 Å)