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Literature summary for 2.7.11.1 extracted from

  • Calamaras, T.; Lee, C.; Lan, F.; Ido, Y.; Siwik, D.; Colucci, W.
    Post-translational modification of serine/threonine kinase LKB1 via adduction of the reactive lipid species 4-hydroxy-trans-2-nonenal (HNE) at lysine residue 97 directly inhibits kinase activity (2012), J. Biol. Chem., 287, 42400-42406.
    View publication on PubMedView publication on EuropePMC
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Activating Compound

Activating Compound Comment Organism Structure
additional information The pseudokinase sterile-20-related adaptor (STRAD) enhances the cytosolic localization of LKB1 and its catalytic activity by acting as an adaptor between exportins (CRM1 and exportin7) and LKB1 Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant GST-tagged LBK1s in HEK-293T cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
K96R the mutant is less sensitive to inhibition by 4-hydroxy-trans-2-nonenal compared to the wild-type Homo sapiens
K96R/K97R the mutant is less sensitive to inhibition by 4-hydroxy-trans-2-nonenal compared to the wild-type and to a greater extent than the single point mutants K96R and K97R Homo sapiens
K97R the mutant is less sensitive to inhibition by 4-hydroxy-trans-2-nonenal compared to the wild-type Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-hydroxy-trans-2-nonenal i.e. 4-HNE, binds to the enzyme at Lys197 and inhibits its activity by 69% by inhibiting its posttranslational phosphorylation. 4-HNE binding has no effect on the association of LKB1 with its adaptor proteins, sterile-20-related adaptor and mouse protein 25 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol active enzyme form, under basal conditions, LKB1 is localized to the nucleus where it has limited catalytic activity. The pseudokinase sterile-20-related adaptor (STRAD) enhances the cytosolic localization of LKB1 by acting as an adaptor between exportins (CRM1 and exportin7) and LKB1 Homo sapiens 5829
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nucleus under basal conditions, LKB1 is localized to the nucleus where it has limited catalytic activity compared to the cytosolic form Homo sapiens 5634
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant wild-type and mutant GST-tagged LBK1s from HEK-293T cells by immunoprecipitation Homo sapiens

Synonyms

Synonyms Comment Organism
LKB1
-
 Homo sapiens
serine/threonine kinase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

General Information

General Information Comment Organism
physiological function LKB1 is a key signaling kinase that regulates cellular growth Homo sapiens