AMPK subfamily

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Enzymes
Kinases (EC 2.7.x.x)
CAMK: Calcium/calmodulin-dependent protein kinases
CAMK-like (CAMKL) family
AMPK subfamily

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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AMP-activated protein kinase (AMPK) is a central regulator of energy homeostasis. Activators that are selective for human AMPKβ2-containing heterotrimers that are expressed in skeletal muscle and liver, are being examined as a novel option to treat metabolic disorders including NASH and diabetes [3,6].

Enzymes

AMPK (AMP kinase) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1540

Nomenclature

AMP kinase

Common abbreviation

AMPK

Previous and unofficial names

AMP-activated protein kinase

EC number

2.7.11.1

Endogenous activators

adenosine 5'-monophosphate pEC₅₀ 4.2 [1]

Selective activators

acadesine [2]

Selective inhibitors

dorsomorphin pIC₅₀ 7.4 [4]

Comment

AMP-activated protein kinase is a heterotrimeric protein kinase, made up of one α, one β and one γ subunit.

AMPKA1 (protein kinase AMP-activated catalytic subunit alpha 1) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1541

Nomenclature

protein kinase AMP-activated catalytic subunit alpha 1

Common abbreviation

AMPKA1

Previous and unofficial names

Genes

PRKAA1 (Hs), Prkaa1 (Mm), Prkaa1 (Rn)

Ensembl ID

ENSG00000132356 (Hs), ENSMUSG00000050697 (Mm), ENSRNOG00000012799 (Rn)

UniProtKB AC

Q13131 (Hs), Q5EG47 (Mm), P54645 (Rn)

EC number

2.7.11.1

AMPKA2 (protein kinase AMP-activated catalytic subunit alpha 2) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1542

Nomenclature

protein kinase AMP-activated catalytic subunit alpha 2

Common abbreviation

AMPKA2

Previous and unofficial names

Genes

PRKAA2 (Hs), Prkaa2 (Mm), Prkaa2 (Rn)

Ensembl ID

ENSG00000162409 (Hs), ENSMUSG00000028518 (Mm), ENSRNOG00000007706 (Rn)

UniProtKB AC

P54646 (Hs), Q8BRK8 (Mm), Q09137 (Rn)

EC number

2.7.11.1

AMPKB1 (protein kinase AMP-activated non-catalytic subunit beta 1) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1543

Nomenclature

protein kinase AMP-activated non-catalytic subunit beta 1

Common abbreviation

AMPKB1

Previous and unofficial names

AMPK beta 1 | 5'-AMP-activated protein kinase 40 kDa subunit | AMPKb | protein kinase, AMP-activated, beta 1 non-catalytic subunit | protein kinase

Genes

PRKAB1 (Hs), Prkab1 (Mm), Prkab1 (Rn)

Ensembl ID

ENSG00000111725 (Hs), ENSMUSG00000029513 (Mm), ENSRNOG00000001142 (Rn)

UniProtKB AC

Q9Y478 (Hs), Q9R078 (Mm), P80386 (Rn)

Activators

MT47-100 pK_i 5.4 [5]

AMPKB2 (protein kinase AMP-activated non-catalytic subunit beta 2) Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1544

Nomenclature

protein kinase AMP-activated non-catalytic subunit beta 2

Common abbreviation

AMPKB2

Previous and unofficial names

AMP-activated protein kinase beta-2 regulatory subunit | AMPK subunit beta-2 | protein kinase

Genes

PRKAB2 (Hs), Prkab2 (Mm), Prkab2 (Rn)

Ensembl ID

ENSG00000131791 (Hs), ENSMUSG00000038205 (Mm), ENSRNOG00000018166 (Rn)

UniProtKB AC

O43741 (Hs), Q7TQI6 (Mm), Q6AYZ8 (Rn)

Allosteric modulators

MT47-100 (Negative) pK_i 4.6 [5]

AMPKG1 (protein kinase AMP-activated non-catalytic subunit gamma 1) Show summary »« Hide summary More detailed page go icon to follow link

Target Id	1545
Nomenclature	protein kinase AMP-activated non-catalytic subunit gamma 1
Common abbreviation	AMPKG1
Previous and unofficial names	Prkga1 \| Prkaac \| protein kinase, AMP-activated, gamma 1 non-catalytic subunit \| AMPK subunit gamma-1 \| AMPKg \| protein kinase
Genes	PRKAG1 (Hs), Prkag1 (Mm), Prkag1 (Rn)
Ensembl ID	ENSG00000181929 (Hs), ENSMUSG00000067713 (Mm), ENSRNOG00000061499 (Rn), ENSRNOG00000070180 (Rn)
UniProtKB AC	P54619 (Hs), O54950 (Mm), P80385 (Rn)

AMPKG2 (protein kinase AMP-activated non-catalytic subunit gamma 2) Show summary »« Hide summary More detailed page go icon to follow link

Target Id	1546
Nomenclature	protein kinase AMP-activated non-catalytic subunit gamma 2
Common abbreviation	AMPKG2
Previous and unofficial names	protein kinase, AMP-activated, gamma 2 non-catalytic subunit \| AMPK subunit gamma-2 \| AAKG \| AAKG2 \| CMH6 \| WPWS \| protein kinase
Genes	PRKAG2 (Hs), Prkag2 (Mm), Prkag2 (Rn)
Ensembl ID	ENSG00000106617 (Hs), ENSMUSG00000028944 (Mm), ENSRNOG00000009085 (Rn)
UniProtKB AC	Q9UGJ0 (Hs), Q91WG5 (Mm)

AMPKG3 (protein kinase AMP-activated non-catalytic subunit gamma 3) Show summary »« Hide summary More detailed page go icon to follow link

Target Id	1547
Nomenclature	protein kinase AMP-activated non-catalytic subunit gamma 3
Common abbreviation	AMPKG3
Previous and unofficial names	protein kinase, AMP-activated, gamma 3 non-catalytic subunit \| Ampkg3 \| AMPK subunit gamma-3 \| protein kinase, AMP-activated, gamma 3 non-catatlytic subunit \| protein kinase
Genes	PRKAG3 (Hs), Prkag3 (Mm), Prkag3 (Rn)
Ensembl ID	ENSG00000115592 (Hs), ENSMUSG00000006542 (Mm), ENSRNOG00000017248 (Rn)
UniProtKB AC	Q9UGI9 (Hs), Q8BGM7 (Mm)

References

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1. Cool B, Zinker B, Chiou W, Kifle L, Cao N, Perham M, Dickinson R, Adler A, Gagne G, Iyengar R et al.. (2006) Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab, 3 (6): 403-16. [PMID:16753576]

2. Corton JM, Gillespie JG, Hawley SA, Hardie DG. (1995) 5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells?. Eur J Biochem, 229 (2): 558-65. [PMID:7744080]

3. Garcia D, Hellberg K, Chaix A, Wallace M, Herzig S, Badur MG, Lin T, Shokhirev MN, Pinto AFM, Ross DS et al.. (2019) Genetic Liver-Specific AMPK Activation Protects against Diet-Induced Obesity and NAFLD. Cell Rep, 26 (1): 192-208.e6. [PMID:30605676]

4. Machrouhi F, Ouhamou N, Laderoute K, Calaoagan J, Bukhtiyarova M, Ehrlich PJ, Klon AE. (2010) The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity. Bioorg Med Chem Lett, 20 (22): 6394-9. [PMID:20932747]

5. Scott JW, Galic S, Graham KL, Foitzik R, Ling NX, Dite TA, Issa SM, Langendorf CG, Weng QP, Thomas HE et al.. (2015) Inhibition of AMP-Activated Protein Kinase at the Allosteric Drug-Binding Site Promotes Islet Insulin Release. Chem Biol, 22 (6): 705-11. [PMID:26091167]

6. Steinberg GR, Carling D. (2019) AMP-activated protein kinase: the current landscape for drug development. Nat Rev Drug Discov, 18 (7): 527-551. [PMID:30867601]

How to cite this family page

Database page citation:

AMPK subfamily. Accessed on 09/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=474.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.