Structure of PDB 5uuu Chain A

Receptor sequence
>5uuuA (length=414) Species: 9606 (Homo sapiens) [Search protein sequence]
KILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRDFCLNNLRGDV
FQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRKA
DTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVCMSYAF
HTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAEIILGLEHMHNR
FVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPEV
LQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAV
ELPDSFSPELRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMV
FLQKYPPPLIPPRGEVEDTKGIKLLDSDQELYRNFPLTISERWQQEVAET
VFDTINAETDRLEA
3D structure
PDB5uuu Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.
ChainA
Resolution2.7 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) D317 K319 N322 D335 K344 T353
Catalytic site (residue number reindexed from 1) D206 K208 N211 D224 K233 T242
Enzyme Commision number 2.7.11.15: [beta-adrenergic-receptor] kinase.
Interaction with ligand
Site
#		 Ligand Ligand
chain		 Binding residues on receptor
(original residue number in PDB)		 Binding residues on receptor
(residue number reindexed from 1)		 Binding affinity
BS01 QRW A R199 G200 F202 G203 V205 A218 K220 L222 L235 A236 E239 M274 L324 G337 R88 G89 F91 G92 V94 A107 K109 L111 L124 A125 E128 M163 L213 G226 PDBbind-CN: -logKd/Ki=7.74,IC50=18nM
BindingDB: EC50=10000nM,IC50=18nM
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004674 protein serine/threonine kinase activity
GO:0004703 G protein-coupled receptor kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation
GO:0007165 signal transduction

View graph for
Molecular Function
View graph for
Biological Process
External links
PDB RCSB:5uuu, PDBe:5uuu, PDBj:5uuu
PDBsum5uuu
PubMed28699740
UniProtP25098|ARBK1_HUMAN Beta-adrenergic receptor kinase 1 (Gene Name=GRK2)

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