Structure of PDB 8uap Chain A

Receptor sequence
>8uapA (length=501) Species: 9606 (Homo sapiens) [Search protein sequence]
GKSKKWKEILKFPHISQCEDLRRTIDRDYCSLCDKQPIGRLLFRQFCETR
PGLECYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFIAQVGQD
LVSQTEEKLLQKPCKELFSACAQSVHEYLRGEPFHEYLDSMFFDRFLQWK
WLERQPVTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKK
RKGESMALNEKQILEKVNSQFVVNLAYAYETKDALCLVLTIMNGGDLKFH
IYNMGNPGFEEERALFYAAEILCGLEDLHRENTVYRNLKPENILLDDYGH
IRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQRYGLSPDYWGLGCL
IYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSICKMLL
TKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYC
DHTDDDFYSKFSTGSVSIPWQNEMIETECFKELNVFGPNGTLPPDLNRNH
P
3D structure
PDB8uap Development of a new class of potent and highly selective G protein-coupled receptor kinase 5 inhibitors and structural insight from crystal structures of inhibitor complexes.
ChainA
Resolution2.5 Å
3D
structure
[Spin on]
[Spin off]
[Reset orientation]

[High quality]
[Low quality]

[White background]
[Black background]

[Download]
[Download structure with residue number starting from 1]
Enzymatic activity
Enzyme Commision number 2.7.11.16: [G-protein-coupled 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 W2T A L192 K194 G195 G198 V200 K215 L263 M266 L318 D329 V472 Y473 L168 K170 G171 G174 V176 K191 L239 M242 L294 D305 V448 Y449
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:0005080 protein kinase C binding
GO:0005515 protein binding
GO:0005524 ATP binding
GO:0005543 phospholipid binding
GO:0008289 lipid binding
GO:0047696 beta-adrenergic receptor kinase activity
Biological Process
GO:0006468 protein phosphorylation
GO:0006915 apoptotic process
GO:0007165 signal transduction
GO:0007186 G protein-coupled receptor signaling pathway
GO:0007188 adenylate cyclase-modulating G protein-coupled receptor signaling pathway
GO:0007217 tachykinin receptor signaling pathway
GO:0008277 regulation of G protein-coupled receptor signaling pathway
GO:0008284 positive regulation of cell population proliferation
GO:0009966 regulation of signal transduction
GO:0016055 Wnt signaling pathway
GO:0016310 phosphorylation
GO:0043066 negative regulation of apoptotic process
GO:0045444 fat cell differentiation
GO:0046777 protein autophosphorylation
GO:0051726 regulation of cell cycle
Cellular Component
GO:0005634 nucleus
GO:0005737 cytoplasm
GO:0005829 cytosol
GO:0005886 plasma membrane
GO:0016607 nuclear speck
GO:0031965 nuclear membrane

View graph for
Molecular Function
View graph for
Biological Process
View graph for
Cellular Component
External links
PDB RCSB:8uap, PDBe:8uap, PDBj:8uap
PDBsum8uap
PubMed38016297
UniProtP34947|GRK5_HUMAN G protein-coupled receptor kinase 5 (Gene Name=GRK5)

[Back to BioLiP]