Target Information

Target General Infomation
Target ID
T74952
Former ID
TTDR00978
Target Name
CAMP-dependent protein kinase type II-beta regulatory chain
Gene Name
PRKAR2B
Synonyms
PKA RIIbeta-subunit; RIIbeta subunit of cAMP-dependent protein kinase; Type RIIbeta regulatory subunit of protein kinase A; PRKAR2B
Target Type
Discontinued
Function
Regulatory subunit of the cAMP-dependent protein kinases involved in cAMP signaling in cells. Type II regulatory chains mediate membrane association by binding to anchoring proteins, including the MAP2 kinase.
BioChemical Class
Kinase
Target Validation
T74952
UniProt ID
P31323
EC Number
EC 2.7.1.37
Sequence
MSIEIPAGLTELLQGFTVEVLRHQPADLLEFALQHFTRLQQENERKGTARFGHEGRTWGD
LGAAAGGGTPSKGVNFAEEPMQSDSEDGEEEEAAPADAGAFNAPVINRFTRRASVCAEAY
NPDEEEDDAESRIIHPKTDDQRNRLQEACKDILLFKNLDPEQMSQVLDAMFEKLVKDGEH
VIDQGDDGDNFYVIDRGTFDIYVKCDGVGRCVGNYDNRGSFGELALMYNTPRAATITATS
PGALWGLDRVTFRRIIVKNNAKKRKMYESFIESLPFLKSLEFSERLKVVDVIGTKVYNDG
EQIIAQGDSADSFFIVESGEVKITMKRKGKSEVEENGAVEIARCSRGQYFGELALVTNKP
RAASAHAIGTVKCLAMDVQAFERLLGPCMEIMKRNIATYEEQLVALFGTNMDIVEPTA
Drugs and Mode of Action
Drug(s) BALANOL Drug Info Terminated Discovery agent [542983], [545589]
Inhibitor 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Drug Info [528490]
AdcAhxArg4Lys(biotin)-PEG-OMe Drug Info [526704]
AdcAhxArg4Lys-PEGOMe Drug Info [526704]
AdcAhxArg4NH(CH2)6NH2 Drug Info [526704]
AdcAhxArg6 Drug Info [526704]
AdoC(Ahx)Arg6 Drug Info [525511]
AdoC(Aoc)Arg6 Drug Info [525511]
AdoC(Aun)Arg6 Drug Info [525511]
AdoC(beta-Ala)2AlaArg6 Drug Info [525511]
AdoC(beta-Ala)Arg6 Drug Info [525511]
AdoC(betaAsp)2AlaArg6 Drug Info [525511]
AdoC(Dpr)2AlaArg6 Drug Info [525511]
AdoC(GABA)Arg6 Drug Info [525511]
AdoCGlyArg6 Drug Info [525511]
BALANOL Drug Info [527710]
Cyclic Adenosine Monophosphate Drug Info [551393]
Ro-4396686 Drug Info [528018]
Pathways
KEGG Pathway Apoptosis
Insulin signaling pathway
PANTHER Pathway Endothelin signaling pathway
Hedgehog signaling pathway
Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Metabotropic glutamate receptor group III pathway
Metabotropic glutamate receptor group II pathway
Muscarinic acetylcholine receptor 2 and 4 signaling pathway
Transcription regulation by bZIP transcription factor
5HT1 type receptor mediated signaling pathway
Beta1 adrenergic receptor signaling pathway
Beta2 adrenergic receptor signaling pathway
Histamine H2 receptor mediated signaling pathway
GABA-B receptor II signaling
Dopamine receptor mediated signaling pathway
Enkephalin release
Reactome PKA activation
PKA activation in glucagon signalling
DARPP-32 events
Regulation of PLK1 Activity at G2/M Transition
Loss of Nlp from mitotic centrosomes
Recruitment of mitotic centrosome proteins and complexes
Loss of proteins required for interphase microtubule organization?from the centrosome
Glucagon-like Peptide-1 (GLP1) regulates insulin secretion
Vasopressin regulates renal water homeostasis via Aquaporins
Hedgehog &#039
off&#039
state
Anchoring of the basal body to the plasma membrane
Factors involved in megakaryocyte development and platelet production
WikiPathways SIDS Susceptibility Pathways
Calcium Regulation in the Cardiac Cell
G Protein Signaling Pathways
Myometrial Relaxation and Contraction Pathways
DAG and IP3 signaling
Regulation of Water Balance by Renal Aquaporins
miRs in Muscle Cell Differentiation
Opioid Signalling
Mitotic G2-G2/M phases
Integration of energy metabolism
Factors involved in megakaryocyte development and platelet production
References
Ref 542983(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8142).
Ref 545589Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003814)
Ref 525511Bioorg Med Chem Lett. 1999 May 17;9(10):1447-52.Adenosine-5'-carboxylic acid peptidyl derivatives as inhibitors of protein kinases.
Ref 526704Bioorg Med Chem Lett. 2003 Sep 15;13(18):3035-9.Liquid-phase synthesis of a pegylated adenosine-oligoarginine conjugate, cell-permeable inhibitor of cAMP-dependent protein kinase.
Ref 527710J Med Chem. 2005 Sep 8;48(18):5613-38.Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.
Ref 528018Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.
Ref 528490J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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