Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: cAMP-dependent protein kinase A type I (PRKAR1A)
• Synonyms: cAMP-dependent protein kinase type I-alpha regulatory subunit; Tissue-specific extinguisher 1; TSE1; PRKAR1; PKR1
• Gene Name: PRKAR1A
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Kinase
• UniProt ID: KAP0_HUMAN
• TTD ID: T08813
• Sequence:
  MESGSTAASEEARSLRECELYVQKHNIQALLKDSIVQLCTARPERPMAFLREYFERLEKE
  EAKQIQNLQKAGTRTDSREDEISPPPPNPVVKGRRRRGAISAEVYTEEDAASYVRKVIPK
  DYKTMAALAKAIEKNVLFSHLDDNERSDIFDAMFSVSFIAGETVIQQGDEGDNFYVIDQG
  ETDVYVNNEWATSVGEGGSFGELALIYGTPRAATVKAKTNVKLWGIDRDSYRRILMGSTL
  RKRKMYEEFLSKVSILESLDKWERLTVADALEPVQFEDGQKIVVQGEPGDEFFIILEGSA
  AVLQRRSENEEFVEVGRLGPSDYFGEIALLMNRPRAATVVARGPLKCVKLDRPRFERVLG
  PCSDILKRNIQQYNSFVSLSV
• Function: Regulatory subunit of the cAMP-dependent protein kinases involved in cAMP signaling in cells.
• KEGG Pathway:
  Apoptosis (hsa04210)
  Insulin signaling pathway (hsa04910)
• Reactome Pathway:
  PKA activation in glucagon signalling (R-HSA-164378)
  DARPP-32 events (R-HSA-180024)
  Glucagon-like Peptide-1 (GLP1) regulates insulin secretion (R-HSA-381676)
  Vasopressin regulates renal water homeostasis via Aquaporins (R-HSA-432040)
  Hedgehog 'off' state (R-HSA-5610787)
  Factors involved in megakaryocyte development and platelet production (R-HSA-983231)
  PKA activation (R-HSA-163615)

Molecular Interaction Atlas (MIA) of This DTT

18 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
5-(2-methylpiperazin-1-ylsulfonyl)isoquinoline	DMV3KBE	Discovery agent	N.A.	Investigative	[2]
AdcAhxArg4Lys(biotin)-PEG-OMe	DMZYJHV	Discovery agent	N.A.	Investigative	[3]
AdcAhxArg4Lys-PEGOMe	DMQ2C8X	Discovery agent	N.A.	Investigative	[3]
AdcAhxArg4NH(CH2)6NH2	DMSYMRJ	Discovery agent	N.A.	Investigative	[3]
AdcAhxArg6	DM7J3K0	Discovery agent	N.A.	Investigative	[3]
AdoC(Ahx)Arg6	DMW5HO0	Discovery agent	N.A.	Investigative	[4]
AdoC(Aoc)Arg6	DMRSCO2	Discovery agent	N.A.	Investigative	[4]
AdoC(Aun)Arg6	DMDLHAB	Discovery agent	N.A.	Investigative	[4]
AdoC(beta-Ala)2AlaArg6	DMPUAFC	Discovery agent	N.A.	Investigative	[4]
AdoC(beta-Ala)Arg6	DMO8D4V	Discovery agent	N.A.	Investigative	[4]
AdoC(betaAsp)2AlaArg6	DM65B7Y	Discovery agent	N.A.	Investigative	[4]
AdoC(Dpr)2AlaArg6	DM2TWSZ	Discovery agent	N.A.	Investigative	[4]
AdoC(GABA)Arg6	DMMWNPT	Discovery agent	N.A.	Investigative	[4]
AdoCGlyArg6	DMVQJP0	Discovery agent	N.A.	Investigative	[4]
Cyclic Guanosine Monophosphate	DMOU93V	Discovery agent	N.A.	Investigative	[1]
RO-316233	DMAGLPW	Discovery agent	N.A.	Investigative	[5]
Sp-Adenosine-3',5'-Cyclic-Monophosphorothioate	DM1VQ4K	Discovery agent	N.A.	Investigative	[1]
[3H]cAMP	DMZRQU7	Discovery agent	N.A.	Investigative	[1]

References

• [1] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [2] Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and... J Biol Chem. 1996 Oct 18;271(42):26157-64.
• [3] Liquid-phase synthesis of a pegylated adenosine-oligoarginine conjugate, cell-permeable inhibitor of cAMP-dependent protein kinase. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3035-9.
• [4] Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases. Bioorg Med Chem Lett. 1999 May 17;9(10):1447-52.
• [5] Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.