Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTW4Y2M)

• DTT Name: cAMP protein kinase type II-beta (PRKAR2B)
• Synonyms: cAMP-dependent protein kinase type II-beta regulatory subunit; Type RIIbeta regulatory subunit of protein kinase A; RIIbeta subunit of cAMP-dependent protein kinase; PKA RIIbeta-subunit
• Gene Name: PRKAR2B
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Kinase
• UniProt ID: KAP3_HUMAN
• TTD ID: T74952
• Sequence:
  MSIEIPAGLTELLQGFTVEVLRHQPADLLEFALQHFTRLQQENERKGTARFGHEGRTWGD
  LGAAAGGGTPSKGVNFAEEPMQSDSEDGEEEEAAPADAGAFNAPVINRFTRRASVCAEAY
  NPDEEEDDAESRIIHPKTDDQRNRLQEACKDILLFKNLDPEQMSQVLDAMFEKLVKDGEH
  VIDQGDDGDNFYVIDRGTFDIYVKCDGVGRCVGNYDNRGSFGELALMYNTPRAATITATS
  PGALWGLDRVTFRRIIVKNNAKKRKMYESFIESLPFLKSLEFSERLKVVDVIGTKVYNDG
  EQIIAQGDSADSFFIVESGEVKITMKRKGKSEVEENGAVEIARCSRGQYFGELALVTNKP
  RAASAHAIGTVKCLAMDVQAFERLLGPCMEIMKRNIATYEEQLVALFGTNMDIVEPTA
• Function: Type II regulatory chains mediate membrane association by binding to anchoring proteins, including the MAP2 kinase. Regulatory subunit of the cAMP-dependent protein kinases involved in cAMP signaling in cells.
• Reactome Pathway:
  PKA activation in glucagon signalling (R-HSA-164378)
  DARPP-32 events (R-HSA-180024)
  Regulation of PLK1 Activity at G2/M Transition (R-HSA-2565942)
  Loss of Nlp from mitotic centrosomes (R-HSA-380259)
  Recruitment of mitotic centrosome proteins and complexes (R-HSA-380270)
  Loss of proteins required for interphase microtubule organization?from the centrosome (R-HSA-380284)
  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)
  Anchoring of the basal body to the plasma membrane (R-HSA-5620912)
  Factors involved in megakaryocyte development and platelet production (R-HSA-983231)
  PKA activation (R-HSA-163615)

Molecular Interaction Atlas (MIA) of This DTT

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BALANOL	DMDLN9E	N. A.	N. A.	Terminated	[1]

16 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol	DMSKJ1X	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]
Ro-4396686	DM5DMCH	Discovery agent	N.A.	Investigative	[5]
[3H]cAMP	DMZRQU7	Discovery agent	N.A.	Investigative	[6]

References

• [1] Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. J Med Chem. 2005 Sep 8;48(18):5613-38. Address
• [2] 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
• [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] Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3.
• [6] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.