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protein kinase, cAMP-dependent, catalytic, beta subunit

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Target not currently curated in GtoImmuPdb

Target id: 1477

Nomenclature: protein kinase, cAMP-dependent, catalytic, beta subunit

Abbreviated Name: PKACb

Family: Protein kinase A (PKA) family

Contents:

Quaternary Structure: Complexes
protein kinase A
Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 351 1p31.1 PRKACB protein kinase cAMP-activated catalytic subunit beta
Mouse - 351 3 H2 Prkacb protein kinase, cAMP dependent, catalytic, beta
Rat - 351 2q44 Prkacb protein kinase cAMP-activated catalytic subunit beta
Previous and Unofficial Names Click here for help
PKA C-beta | cAMP-dependent protein kinase C beta | protein kinase, cAMP-dependent, catalytic, beta | protein kinase, cAMP-dependent, beta catalytic subunit | protein kinase
Database Links Click here for help
Alphafold P22694 (Hs), P68181 (Mm), P68182 (Rn)
BRENDA 2.7.11.11
ChEMBL Target CHEMBL2918 (Hs)
Ensembl Gene ENSG00000142875 (Hs), ENSMUSG00000005034 (Mm), ENSRNOG00000004978 (Rn)
Entrez Gene 5567 (Hs), 18749 (Mm), 293508 (Rn)
Human Protein Atlas ENSG00000142875 (Hs)
KEGG Enzyme 2.7.11.11
KEGG Gene hsa:5567 (Hs), mmu:18749 (Mm), rno:293508 (Rn)
OMIM 176892 (Hs)
Pharos P22694 (Hs)
RefSeq Nucleotide NM_001242857 (Hs), NM_011100 (Mm), NM_001077645 (Rn)
RefSeq Protein NP_002722 (Hs), NP_035230 (Mm), NP_001157670 (Mm), NP_001157671 (Mm), NP_001157672 (Mm), NP_001071113 (Rn)
UniProtKB P22694 (Hs), P68181 (Mm), P68182 (Rn)
Wikipedia PRKACB (Hs)
Enzyme Reaction Click here for help
EC Number: 2.7.11.11

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GSK690693 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pKd 1
⤷ pKd 7.9 (Kd 1.3x10-8 M) [1]
staurosporine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 2
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [2]
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: PKAC-beta
Ligand Sp. Type Action Value Parameter
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 6.6 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
enzastaurin Small molecule or natural product Hs Inhibitor Inhibition 6.2 pKd
SB203580 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition <5.5 pKd
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition <5.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Cellular signalling

References

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1. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

2. Djung JF, Mears RJ, Montalbetti CA, Coulter TS, Golebiowski A, Carr AN, Barker O, Greis KD, Zhou S, Dolan E et al.. (2011) The synthesis and evaluation of indolylureas as PKCα inhibitors. Bioorg Med Chem, 19 (8): 2742-50. [PMID:21435888]

3. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Protein kinase A (PKA) family: protein kinase, cAMP-dependent, catalytic, beta subunit. Last modified on 12/04/2019. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1477.