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Literature summary extracted from

  • Brown, T.R.; Su, B.; Brown, K.A.; Schwartz, M.A.; Tobia, A.M.; Kappler, F.
    Modulation of in vivo 3-deoxyglucosone levels (2003), Biochem. Soc. Trans., 31, 1433-1437.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.1.171 medicine inhibition of fructoseamine-3-kinase is a promising new therapeutic target for diabetic complications, as well as other 3-deoxyglucosone-dependent pathologies Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.1.171 3-O-methylsorbitol-lysine inhibitors based on sorbitol show competitive inhibition of the fructoseamine-3-kinase reaction but also prevent the formation of 3-deoxyglucosone, because there is no spontaneous decomposition of the product to 3-deoxyglucosone. For compounds blocked at C3, also there is no product formed. The Ki values of these compounds are approx. 0.5 mM. Although high for an in vivo drug, their apparent low toxicity make it possible to use them, at least in animals, to lower 3-deoxyglucosone levels Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.1.171 ATP + [protein]-N6-D-fructosyl-L-lysine Rattus norvegicus fructoselysine 3-phosphate spontaneously decomposes to lysine, phosphate and 3-deoxyglucosone. This pathway appears to dominate 3-deoxyglucosone production in vivo, making it possible to modulate 3-deoxyglucosone levels by stimulating or inhibiting the reaction ADP + [protein]-N6-(O3-phosphono-D-fructosyl)-L-lysine
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 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.1.171 Rattus norvegicus
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 Sprague–Dawley or Fisher 344. Rats carrying the Tsc2 gene (Eker rats) in a Fisher 344 background
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Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.1.171 blood plasma
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 Rattus norvegicus
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Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.1.171 ATP + [protein]-N6-D-fructosyl-L-lysine
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 Rattus norvegicus ADP + [protein]-N6-(O3-phosphono-D-fructosyl)-L-lysine fructoselysine 3-phosphate spontaneously decomposes to lysine, phosphate and 3-deoxyglucosone ?
2.7.1.171 ATP + [protein]-N6-D-fructosyl-L-lysine fructoselysine 3-phosphate spontaneously decomposes to lysine, phosphate and 3-deoxyglucosone. This pathway appears to dominate 3-deoxyglucosone production in vivo, making it possible to modulate 3-deoxyglucosone levels by stimulating or inhibiting the reaction Rattus norvegicus ADP + [protein]-N6-(O3-phosphono-D-fructosyl)-L-lysine
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 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.1.171 FL3P
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 Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.1.171 additional information
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 3-O-methylsorbitol-lysine inhibitors based on sorbitol show competitive inhibition of the fructoseamine-3-kinase reaction but also prevent the formation of 3-deoxyglucosone, because there is no spontaneous decomposition of the product to 3-deoxyglucosone. For compounds blocked at C3, also there is no product formed. The Ki values of these compounds are approx. 0.5 mM. Although high for an in vivo drug, their apparent low toxicity make it possible to use them, at least in animals, to lower 3-deoxyglucosone levels Rattus norvegicus

Expression

EC Number Organism Comment Expression
2.7.1.171 Rattus norvegicus mildly glycated casein in a standard diet stimulates 3-deoxyglucosone levels 10–20fold in the plasma and approximately 3fold in the kidney compared with a control diet containing identical constituents additional information