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; PRKG2
DTT Type	Literature-reported target	[1]
BioChemical Class	Kinase
UniProt ID	KGP1_HUMAN ; KGP2_HUMAN
TTD ID	T56035
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
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

Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas 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]
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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.