4MK0

Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative

Summary for 4MK0

Entry DOI	10.2210/pdb4mk0/pdb
Related	1OMW 3V5W 4L9I
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	inhibitor complex, protein kinase, hydrolase, atp binding, phosphorylation, peripheral membrane protein, signaling protein-inhibitor complex, signaling protein/inhibitor
Biological source	Homo sapiens (human) More
Cellular location	Cytoplasm : P25098 Cell membrane ; Lipid-anchor ; Cytoplasmic side : P63212
Total number of polymer chains	3
Total formula weight	118781.37
Authors	Homan, K.T.,Tesmer, J.J.G. (deposition date: 2013-09-04, release date: 2014-01-22, Last modification date: 2024-02-28)
Primary citation	Homan, K.T.,Wu, E.,Wilson, M.W.,Singh, P.,Larsen, S.D.,Tesmer, J.J. Structural and functional analysis of g protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog. Mol.Pharmacol., 85:237-248, 2014 Cited by PubMed: 24220010 DOI: 10.1124/mol.113.089631 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.4 Å)

Structure validation