Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTZC6DR)

• DTT Name: cGMP-dependent protein kinase (cGK)
• Synonyms: cGK; PRKGR
• Gene Name: PRKG1
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Kinase
• UniProt ID: KGP1_HUMAN ; KGP2_HUMAN
• TTD ID: T56035
• Sequence:
  MSELEEDFAKILMLKEERIKELEKRLSEKEEEIQELKRKLHKCQSVLPVPSTHIGPRTTR
  AQGISAEPQTYRSFHDLRQAFRKFTKSERSKDLIKEAILDNDFMKNLELSQIQEIVDCMY
  PVEYGKDSCIIKEGDVGSLVYVMEDGKVEVTKEGVKLCTMGPGKVFGELAILYNCTRTAT
  VKTLVNVKLWAIDRQCFQTIMMRTGLIKHTEYMEFLKSVPTFQSLPEEILSKLADVLEET
  HYENGEYIIRQGARGDTFFIISKGTVNVTREDSPSEDPVFLRTLGKGDWFGEKALQGEDV
  RTANVIAAEAVTCLVIDRDSFKHLIGGLDDVSNKAYEDAEAKAKYEAEAAFFANLKLSDF
  NIIDTLGVGGFGRVELVQLKSEESKTFAMKILKKRHIVDTRQQEHIRSEKQIMQGAHSDF
  IVRLYRTFKDSKYLYMLMEACLGGELWTILRDRGSFEDSTTRFYTACVVEAFAYLHSKGI
  IYRDLKPENLILDHRGYAKLVDFGFAKKIGFGKKTWTFCGTPEYVAPEIILNKGHDISAD
  YWSLGILMYELLTGSPPFSGPDPMKTYNIILRGIDMIEFPKKIAKNAANLIKKLCRDNPS
  ERLGNLKNGVKDIQKHKWFEGFNWEGLRKGTLTPPIIPSVASPTDTSNFDSFPEDNDEPP
  PDDNSGWDIDF
• Function: Activated by cGMP. Phosphorylates a number of biologically important targets and is implicated in the regulation of smooth muscle relaxation, platelet function, sperm metabolism, cell division, and nucleic acid synthesis.
• KEGG Pathway:
  cGMP-PKG signaling pathway (hsa04022)
  Vascular smooth muscle contraction (hsa04270)
  Gap junction (hsa04540)
  Platelet activation (hsa04611)
  Circadian entrainment (hsa04713)
  Thermogenesis (hsa04714)
  Long-term depression (hsa04730)
  Olfactory transduction (hsa04740)
  Regulation of lipolysis in adipocytes (hsa04923)
  Salivary secretion (hsa04970)
• Reactome Pathway:
  Ca2+ pathway (R-HSA-4086398)
  cGMP effects (R-HSA-418457)
  Rap1 signalling (R-HSA-392517)

Molecular Interaction Atlas (MIA) of This DTT

4 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ARC-1028	DM0KDTG	Discovery agent	N.A.	Investigative	[2]
STAUROSPORINONE	DMU2H4K	Discovery agent	N.A.	Investigative	[1]
TENELLONE A	DM1S209	Discovery agent	N.A.	Investigative	[3]
TENELLONE B	DM9ZVJ7	Discovery agent	N.A.	Investigative	[3]

References

• [1] Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C, Bioorg. Med. Chem. Lett. 3(10):1959-1964 (1993).
• [2] Structural analysis of ARC-type inhibitor (ARC-1034) binding to protein kinase A catalytic subunit and rational design of bisubstrate analogue inhi... J Med Chem. 2009 Jan 22;52(2):308-21.
• [3] Tenellones A and B from a Diaporthe sp.: two highly substituted benzophenone inhibitors of parasite cGMP-dependent protein kinase activity. J Nat Prod. 2005 Apr;68(4):611-3.