4WNP

Structure of ULK1 bound to a potent inhibitor

4WNP の概要

• エントリーDOI: 10.2210/pdb4wnp/pdb
• 関連するPDBエントリー: 4WNO
• 分子名称: Serine/threonine-protein kinase ULK1, GLYCEROL, N~2~-(1H-benzimidazol-6-yl)-N~4~-(5-cyclobutyl-1H-pyrazol-3-yl)quinazoline-2,4-diamine, ... (4 entities in total)
• 機能のキーワード: kinase, autophagy, inhibitor, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Cytoplasm, cytosol : O75385
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 131051.03

構造登録者

Lazarus, M.B.,Novotny, C.J.,Shokat, K.M. (登録日: 2014-10-14, 公開日: 2015-01-14, 最終更新日: 2024-11-13)

主引用文献

Lazarus, M.B.,Novotny, C.J.,Shokat, K.M.
Structure of the Human Autophagy Initiating Kinase ULK1 in Complex with Potent Inhibitors.
Acs Chem.Biol., 10:257-261, 2015

PubMed Abstract: Autophagy is a conserved cellular process that involves the degradation of cellular components for energy maintenance and cytoplasmic quality control that has recently gained interest as a novel target for a variety of human diseases, including cancer. A prime candidate to determine the potential therapeutic benefit of targeting autophagy is the kinase ULK1, whose activation initiates autophagy. Here, we report the first structures of ULK1, in complex with multiple potent inhibitors. These structures show features unique to the enzyme and will provide a path for the rational design of selective compounds as cellular probes and potential therapeutics.

PubMed: 25551253
DOI: 10.1021/cb500835z

実験手法

X-RAY DIFFRACTION (1.88 Å)