protein kinase A | Protein kinase A (PKA) family | IUPHAR/BPS Guide to PHARMACOLOGY

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protein kinase A

Target not currently curated in GtoImmuPdb

Target id: 1694

Nomenclature: protein kinase A

Family: Protein kinase A (PKA) family

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

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
ATP:protein phosphotransferase (cAMP-dependent) | STK22
Database Links
BRENDA
KEGG Enzyme
Enzyme Reaction
EC Number: 2.7.11.11

Download all structure-activity data for this target as a CSV file

Activators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]cAMP Hs Activation - -
N6 benzyl-cAMP Hs Activation - - 1
[1]
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
balanol 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] Hs Inhibition 9.5 pIC50 3
pIC50 9.5 (IC50 3x10-10 M) [3]
compound 1 [PMID: 20005102] Hs Inhibition 9.0 pIC50 7
pIC50 9.0 (IC50 1x10-9 M) [7]
BX-912 Hs Inhibition 7.0 pIC50 5
pIC50 7.0 (IC50 1.1x10-7 M) [5]
compound 1 [PMID: 21742770] Hs Inhibition 6.7 pIC50 9
pIC50 6.7 (IC50 1.96x10-7 M) [9]
compound 33 [PMID: 19364658] Hs Inhibition 6.6 pIC50 8
pIC50 6.6 (IC50 2.7x10-7 M) [8]
BX-795 Hs Inhibition 6.1 pIC50 5
pIC50 6.1 (IC50 8.4x10-7 M) [5]
chelerythrine Hs Inhibition 6.1 pIC50 4
pIC50 6.1 (IC50 9x10-7 M) [4]
7-hydroxystaurosporine Rn Inhibition 6.0 pIC50 6
pIC50 6.0 (IC50 1x10-6 M) [6]
Rp-cAMPS Hs 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. U.S.A., 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 25/07/2019. Accessed on 08/12/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1694.