7K7Z

Structure of a hit for G Protein Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure

Summary for 7K7Z

• Entry DOI: 10.2210/pdb7k7z/pdb
• Related: 7k7l
• Descriptor: Beta-adrenergic receptor kinase 1, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... (4 entities in total)
• Functional Keywords: serine/threonine protein kinase, signaling protein, transferase-inhibitor complex, transferase/inhibitor
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 3
• Total formula weight: 118653.23

Authors

Spurlino, J.C.,Milligan, C. (deposition date: 2020-09-24, release date: 2020-10-28, Last modification date: 2024-04-03)

• Primary citation: Xu, G.,Gaul, M.D.,Liu, Z.,DesJarlais, R.L.,Qi, J.,Wang, W.,Krosky, D.,Petrounia, I.,Milligan, C.M.,Hermans, A.,Lu, H.R.,Huang, D.Z.,Xu, J.Z.,Spurlino, J.C.; Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor.; Bioorg.Med.Chem.Lett., 30:127602-127602, 2020; PubMed: 33038544; DOI: 10.1016/j.bmcl.2020.127602

Experimental method

X-RAY DIFFRACTION (2.60608692764 Å)