8UAQ

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

Summary for 8UAQ

• Entry DOI: 10.2210/pdb8uaq/pdb
• Descriptor: 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)
• Functional Keywords: g protein-coupled receptor, gpcr g protein-coupled receptor kinase, grk kinase, signaling protein-inhibitor complex, signaling protein/inhibitor
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 69474.29

Authors

Chen, Y.,Tesmer, J.J.G. (deposition date: 2023-09-21, release date: 2023-12-13)

• Primary citation: 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

Experimental method

X-RAY DIFFRACTION (2.8 Å)