Structure of PDB 5uvc Chain A

Receptor sequence
>5uvcA (length=457) Species: 9606 (Homo sapiens) [Search protein sequence]
KKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRDFCLNHLEEA
RPLVEFYEEIKKYEKLEVARSREIFDSYIMKELLAPPDLFQPYIEEICQN
LRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVY
GCRKADTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVC
MSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAEIILGLE
HMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGY
MAPEVLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMT
LTMAVELPDSFSPELRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSL
DWQMVFLQKYPPPLIPPRGLDSDQELYRNFPLTISERWQQEVAETVFDTI
NAETDRL
3D structure
PDB5uvc 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
Resolution2.65 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) D261 K263 N266 D279 K288 T297
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 8PV A G200 V205 A218 K220 M274 L324 D335 G144 V149 A162 K164 M218 L268 D279 PDBbind-CN: -logKd/Ki=8.21,IC50=6.1nM
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:5uvc, PDBe:5uvc, PDBj:5uvc
PDBsum5uvc
PubMed28699740
UniProtP25098|ARBK1_HUMAN Beta-adrenergic receptor kinase 1 (Gene Name=GRK2)

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