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protein kinase A

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Target not currently curated in GtoImmuPdb

Target id: 1694

Nomenclature: protein kinase A

Family: Protein kinase A (PKA) family

Quaternary Structure: Subunits
protein kinase, cAMP-dependent, regulatory, type I, alpha subunit
protein kinase, cAMP-dependent, regulatory, type I, beta subunit
protein kinase, cAMP-dependent, regulatory, type II, alpha subunit
protein kinase, cAMP-dependent, regulatory, type II, beta subunit
protein kinase, cAMP-dependent, catalytic, alpha subunit
protein kinase, cAMP-dependent, catalytic, beta subunit
protein kinase, cAMP-dependent, catalytic, gamma subunit
Quaternary Structure Comments
The inactive holoenzyme of protein kinase A consists of two regulatory and two catalytic chains.
Previous and Unofficial Names Click here for help
ATP:protein phosphotransferase (cAMP-dependent) | STK22
Database Links Click here for help
BRENDA
KEGG Enzyme
Enzyme Reaction Click here for help
EC Number: 2.7.11.11

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Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]cAMP Small molecule or natural product Ligand is labelled Ligand is radioactive Ligand has a PDB structure Hs Activation - -
N6 benzyl-cAMP Small molecule or natural product Hs Activation - - 1
[1]
Sp-cAMPS Small molecule or natural product N/A Activation - -
View species-specific activator tables
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
balanol Small molecule or natural product Ligand has a PDB structure Rn Inhibition 10.4 pIC50 2
pIC50 10.4 (IC50 4x10-11 M) [2]
Description: Inhibition of PKA extracted from rat brain homogenate.
compound E22 [PMID: 31298542] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.5 pIC50 3
pIC50 9.5 (IC50 3x10-10 M) [3]
compound 1 [PMID: 20005102] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.0 pIC50 7
pIC50 9.0 (IC50 1x10-9 M) [7]
BX-912 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.0 pIC50 5
pIC50 7.0 (IC50 1.1x10-7 M) [5]
compound 1 [PMID: 21742770] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 9
pIC50 6.7 (IC50 1.96x10-7 M) [9]
compound 33 [PMID: 19364658] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.6 pIC50 8
pIC50 6.6 (IC50 2.7x10-7 M) [8]
BX-795 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.1 pIC50 5
pIC50 6.1 (IC50 8.4x10-7 M) [5]
chelerythrine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pIC50 4
pIC50 6.1 (IC50 9x10-7 M) [4]
7-hydroxystaurosporine Small molecule or natural product Ligand has a PDB structure Rn Inhibition 6.0 pIC50 6
pIC50 6.0 (IC50 1x10-6 M) [6]
Rp-cAMPS Small molecule or natural product Ligand has a PDB structure Hs Inhibition - -
myr-PKI Peptide N/A Inhibition - -
View species-specific inhibitor tables

References

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1. Christensen AE, Selheim F, de Rooij J, Dremier S, Schwede F, Dao KK, Martinez A, Maenhaut C, Bos JL, Genieser HG et al.. (2003) cAMP analog mapping of Epac1 and cAMP kinase. Discriminating analogs demonstrate that Epac and cAMP kinase act synergistically to promote PC-12 cell neurite extension. J Biol Chem, 278 (37): 35394-402. [PMID:12819211]

2. Defauw JM, Murphy MM, Jagdmann Jr GE, Hu H, Lampe JW, Hollinshead SP, Mitchell TJ, Crane HM, Heerding JM, Mendoza JS et al.. (1996) Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A. J Med Chem, 39 (26): 5215-27. [PMID:8978850]

3. Dong X, Zhan W, Zhao M, Che J, Dai X, Wu Y, Xu L, Zhou Y, Zhao Y, Tian T et al.. (2019) Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design. J Med Chem, 62 (15): 7264-7288. [PMID:31298542]

4. Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S. (2007) A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci USA, 104 (51): 20523-8. [PMID:18077363]

5. Feldman RI, Wu JM, Polokoff MA, Kochanny MJ, Dinter H, Zhu D, Biroc SL, Alicke B, Bryant J, Yuan S et al.. (2005) Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem, 280 (20): 19867-74. [PMID:15772071]

6. Jiang X, Zhao B, Britton R, Lim LY, Leong D, Sanghera JS, Zhou BB, Piers E, Andersen RJ, Roberge M. (2004) Inhibition of Chk1 by the G2 DNA damage checkpoint inhibitor isogranulatimide. Mol Cancer Ther, 3 (10): 1221-7. [PMID:15486189]

7. Lin H, Yamashita DS, Zeng J, Xie R, Verma S, Luengo JI, Rhodes N, Zhang S, Robell KA, Choudhry AE et al.. (2010) 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles. Bioorg Med Chem Lett, 20 (2): 679-83. [PMID:20005102]

8. Lovering F, Kirincich S, Wang W, Combs K, Resnick L, Sabalski JE, Butera J, Liu J, Parris K, Telliez JB. (2009) Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2). Bioorg Med Chem, 17 (9): 3342-51. [PMID:19364658]

9. Weïwer M, Spoonamore J, Wei J, Guichard B, Ross NT, Masson K, Silkworth W, Dandapani S, Palmer M, Scherer CA et al.. (2012) A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells. ACS Med Chem Lett, 3 (12): 1034-1038. [PMID:23256033]

How to cite this page

Protein kinase A (PKA) family: protein kinase A. Last modified on 27/01/2020. Accessed on 28/10/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1694.