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Literature summary for 2.7.11.31 extracted from

  • Wang, Y.; Viollet, B.; Terkeltaub, R.; Liu-Bryan, R.
    AMP-activated protein kinase suppresses urate crystal-induced inflammation and transduces colchicine effects in macrophages (2016), Ann. Rheum. Dis., 75, 286-294.
    View publication on PubMedView publication on EuropePMC
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Activating Compound

Activating Compound Comment Organism Structure
A-769662 a selective pharmacological activator of AMPK. A-769662 promotes AMPK-dependent macrophage anti-inflammatory M2 polarisation and inhibits NLRP3 gene expression, activation of caspase-1 and IL-1beta Mus musculus
Colchicine at low concentration (10 nM) promotes phosphorylation of AMPKalpha and macrophage M2 polarisation and reduces activation of caspase-1 and release of IL-1beta and CXCL1 by monosodium urate crystals in BMDMs in vitro. Activation of AMPK is induced by certain drugs already in the clinic for arthritis and other diseases (e.g. methotrexate, high-dose aspirin, metformin) and by other agents, including the selective and direct activator A-769661 Mus musculus
additional information phosphorylation on Thr172 and activation of AMPKalpha subunit Mus musculus

Protein Variants

Protein Variants Comment Organism
additional information knockout of AMPKalpha1 subunit Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus Q5EG47
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-
Mus musculus C57BL/6/129 Q5EG47
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-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein phosphorylation on Thr172 and activation of AMPKalpha subunit Mus musculus

Source Tissue

Source Tissue Comment Organism Textmining
bone marrow
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 Mus musculus
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macrophage bone marrow-derived Mus musculus
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Synonyms

Synonyms Comment Organism
5'-AMP-activated protein kinase catalytic subunit alpha-1
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 Mus musculus
AMP-activated protein kinase
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 Mus musculus
AMPK
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 Mus musculus

General Information

General Information Comment Organism
malfunction knockout of AMPKalpha1 enhances, and, conversely, activator A-769662 inhibits monosodium urate crystal-induced inflammatory responses including IL-1beta and CXCL1 release in vitro and in vivo Mus musculus
physiological function AMP-activated protein kinase (AMPK) is metabolic biosensor with anti-inflammatory activities. Gout is commonly associated with excesses in soluble urate and in nutrition, both of which suppress tissue AMPK activity. Gout is driven by macrophage-mediated inflammation transduced partly by NLRP3 inflammasome activation and interleukin-1beta release. AMP-activated protein kinase suppresses urate crystal-induced inflammation and transduces colchicine effects in macrophages. Activated AMPK is anti-inflammatory partly through inhibition of NF-kappaB Mus musculus