3KRW

Human GRK2 in complex with Gbetgamma subunits and balanol (soak)

Summary for 3KRW

• Entry DOI: 10.2210/pdb3krw/pdb
• Related: 1BX6 1OMW 3CIK 3KRX
• 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, ... (6 entities in total)
• Functional Keywords: protein kinase, inhibitor, complex, wd40, ph domain, rgs homology domain, atp-binding, kinase, nucleotide-binding, phosphoprotein, polymorphism, serine/threonine-protein kinase, transferase, acetylation, transducer, wd repeat, cell membrane, lipoprotein, membrane, methylation, prenylation, protein binding
• Biological source: Homo sapiens (human); More
• Cellular location: Cell membrane; Lipid-anchor; Cytoplasmic side (Potential): P63212
• Total number of polymer chains: 3
• Total formula weight: 125959.85

Authors

Tesmer, J.J.G.,Tesmer, V.M. (deposition date: 2009-11-19, release date: 2010-02-16, Last modification date: 2023-09-06)

Primary citation

Tesmer, J.J.,Tesmer, V.M.,Lodowski, D.T.,Steinhagen, H.,Huber, J.
Structure of human g protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
J.Med.Chem., 53:1867-1870, 2010

PubMed Abstract: G protein-coupled receptor kinase 2 (GRK2) is a pharmaceutical target for the treatment of cardiovascular diseases such as congestive heart failure, myocardial infarction, and hypertension. To better understand how nanomolar inhibition and selectivity for GRK2 might be achieved, we have determined crystal structures of human GRK2 in complex with Gbetagamma in the presence and absence of the AGC kinase inhibitor balanol. The selectivity of balanol among human GRKs is assessed.

PubMed: 20128603
DOI: 10.1021/jm9017515

Experimental method

X-RAY DIFFRACTION (2.9 Å)