Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT5A4DX)

• DTT Name: Beta-adrenergic receptor kinase 2 (ADRBK2)
• Synonyms: G-protein-coupled receptor kinase 3; Beta-ARK-2; BARK2; ADRBK2
• Gene Name: GRK3
• DTT Type: Literature-reported target; [1]
• UniProt ID: ARBK2_HUMAN
• TTD ID: T57174
• EC Number: EC 2.7.11.15
• Sequence:
  MADLEAVLADVSYLMAMEKSKATPAARASKRIVLPEPSIRSVMQKYLAERNEITFDKIFN
  QKIGFLLFKDFCLNEINEAVPQVKFYEEIKEYEKLDNEEDRLCRSRQIYDAYIMKELLSC
  SHPFSKQAVEHVQSHLSKKQVTSTLFQPYIEEICESLRGDIFQKFMESDKFTRFCQWKNV
  ELNIHLTMNEFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
  IMLSLVSTGDCPFIVCMTYAFHTPDKLCFILDLMNGGDLHYHLSQHGVFSEKEMRFYATE
  IILGLEHMHNRFVVYRDLKPANILLDEHGHARISDLGLACDFSKKKPHASVGTHGYMAPE
  VLQKGTAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTVNVELPDTFSPE
  LKSLLEGLLQRDVSKRLGCHGGGSQEVKEHSFFKGVDWQHVYLQKYPPPLIPPRGEVNAA
  DAFDIGSFDEEDTKGIKLLDCDQELYKNFPLVISERWQQEVTETVYEAVNADTDKIEARK
  RAKNKQLGHEEDYALGKDCIMHGYMLKLGNPFLTQWQRRYFYLFPNRLEWRGEGESRQNL
  LTMEQILSVEETQIKDKKCILFRIKGGKQFVLQCESDPEFVQWKKELNETFKEAQRLLRR
  APKFLNKPRSGTVELPKPSLCHRNSNGL
• Function: Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors.
• KEGG Pathway:
  Chemokine signaling pathway (hsa04062)
  Endocytosis (hsa04144)
  Hedgehog signaling pathway (hsa04340)
  Glutamatergic synapse (hsa04724)
  Olfactory transduction (hsa04740)
  Morphine addiction (hsa05032)
• Reactome Pathway:
  Cargo recognition for clathrin-mediated endocytosis (R-HSA-8856825)
  G alpha (s) signalling events (R-HSA-418555)

Molecular Interaction Atlas (MIA) of This DTT

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID21596927C101	DM7JRHB	Discovery agent	N.A.	Investigative	[1]

References

• [1] Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol Pharmacol. 2011 Aug;80(2):294-303.