4EQU

Human STK-10 (LOK) kinase domain in DFG-out conformation with inhibitor DSA-7

4EQU の概要

• エントリーDOI: 10.2210/pdb4equ/pdb
• 分子名称: Serine/threonine-protein kinase 10, N-{3-[(3-{4-[(4-methoxyphenyl)amino]-1,3,5-triazin-2-yl}pyridin-2-yl)amino]-4-methylphenyl}-3-(trifluoromethyl)benzamide, CALCIUM ION, ... (5 entities in total)
• 機能のキーワード: serine/threonine kinase, transferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cell membrane; Peripheral membrane protein: O94804
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 70178.98

構造登録者

Merritt, E.A.,Larson, E.T. (登録日: 2012-04-19, 公開日: 2012-11-07, 最終更新日: 2024-11-27)

主引用文献

Ranjitkar, P.,Perera, B.G.,Swaney, D.L.,Hari, S.B.,Larson, E.T.,Krishnamurty, R.,Merritt, E.A.,Villen, J.,Maly, D.J.
Affinity-Based Probes Based on Type II Kinase Inhibitors.
J.Am.Chem.Soc., 134:19017-19025, 2012

PubMed Abstract: Protein kinases are key components of most mammalian signal transduction networks and are therapeutically relevant drug targets. Efforts to study protein kinase function would benefit from new technologies that are able to profile kinases in complex proteomes. Here, we describe active site-directed probes for profiling kinases in whole cell extracts and live cells. These probes contain general ligands that stabilize a specific inactive conformation of the ATP-binding sites of protein kinases, as well as trifluoromethylphenyl diazirine and alkyne moieties that allow covalent modification and enrichment of kinases, respectively. A diverse group of serine/threonine and tyrosine kinases were identified as specific targets of these probes in whole cell extracts. In addition, a number of kinase targets were selectively labeled in live cells. Our chemical proteomics approach should be valuable for interrogating protein kinase active sites in physiologically relevant environments.

PubMed: 23088519
DOI: 10.1021/ja306035v

実験手法

X-RAY DIFFRACTION (2 Å)