8UAQ

Crystal Structure of Human G Protein-Coupled Receptor Kinase 5 in Complex with GRL018-21

8UAQ の概要

• エントリーDOI: 10.2210/pdb8uaq/pdb
• 分子名称: G protein-coupled receptor kinase 5, (3Z)-N-[(1R)-1-(4-fluorophenyl)ethyl]-3-[(4-{[(2S)-2-(furan-2-yl)-2-hydroxyacetyl]amino}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indole-5-carboxamide (3 entities in total)
• 機能のキーワード: g protein-coupled receptor, gpcr g protein-coupled receptor kinase, grk kinase, signaling protein-inhibitor complex, signaling protein/inhibitor
• 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: 69474.29

構造登録者

Chen, Y.,Tesmer, J.J.G. (登録日: 2023-09-21, 公開日: 2023-12-13)

• 主引用文献: Chen, Y.,Sonawane, A.,Manda, R.,Gadi, R.K.,Tesmer, J.J.G.,Ghosh, A.K.; Development of a new class of potent and highly selective G protein-coupled receptor kinase 5 inhibitors and structural insight from crystal structures of inhibitor complexes.; Eur.J.Med.Chem., 264:115931-115931, 2023; PubMed: 38016297; DOI: 10.1016/j.ejmech.2023.115931

実験手法

X-RAY DIFFRACTION (2.8 Å)