7K7L

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

Summary for 7K7L

Entry DOI	10.2210/pdb7k7l/pdb
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, ... (5 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	118677.53
Authors	Spurlino, J.C.,Milligan, C. (deposition date: 2020-09-23, 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 Cited by PubMed: 33038544 DOI: 10.1016/j.bmcl.2020.127602 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.539 Å)

Structure validation