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Literature summary for 1.2.1.105 extracted from

  • Bunik, V.I.; Denton, T.T.; Xu, H.; Thompson, C.M.; Cooper, A.J.; Gibson, G.E.
    Phosphonate analogues of alpha-ketoglutarate inhibit the activity of the alpha-ketoglutarate dehydrogenase complex isolated from brain and in cultured cells (2005), Biochemistry, 44, 10552-10561.
    View publication on PubMed

Application

Application Comment Organism
medicine succinyl phosphonate and its esters may be useful in studying the effects of reduced KGDHC activity on neuronal and brain function Homo sapiens
medicine succinyl phosphonate and its esters may be useful in studying the effects of reduced KGDHC activity on neuronal and brain function Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
4-oxo-4-phosphonobutanoic acid 0.01 mM completely inhibits even in the presence of a 200fold higher concentration of its substrate 2-oxoglutarate Bos taurus
4-oxo-4-phosphonobutanoic acid 0.01 mM produce 70% inhibition Homo sapiens
4-[(2-carboxyethoxy)(hydroxy)phosphoryl]-4-oxobutanoic acid 0.01 mM completely inhibits even in the presence of a 200fold higher concentration of its substrate 2-oxoglutarate Bos taurus
4-[(2-carboxyethoxy)(hydroxy)phosphoryl]-4-oxobutanoic acid 0.01 mM produce 70% inhibition Homo sapiens
4-[ethoxy(hydroxy)phosphoryl]-4-oxobutanoic acid 0.01 mM completely inhibits even in the presence of a 200fold higher concentration of its substrate 2-oxoglutarate Bos taurus
4-[ethoxy(hydroxy)phosphoryl]-4-oxobutanoic acid 0.01 mM produce 70% inhibition Homo sapiens
ethyl 4-[ethoxy(hydroxy)phosphoryl]-4-oxobutanoate only inhibitory after preincubation, release of charged groups by cellular esterases and activation in intact cells Homo sapiens
additional information ethyl 4-[ethoxy(hydroxy)phosphoryl]-4-oxobutanoate and triethyl esters of succinyl phosphonate are ineffective Bos taurus
triethyl ester of succinyl phosphonate only inhibitory after preincubation, release of charged groups by cellular esterases and activation in intact cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Bos taurus

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
Bos taurus
-
culture medium
-
Homo sapiens
-
fibroblast
-
Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.1
-
-
Bos taurus
0.2
-
-
Bos taurus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-oxoglutarate + [dihydrolipoyllysine-residue succinyltransferase] lipoyllysine
-
Bos taurus [dihydrolipoyllysine-residue succinyltransferase] S-succinyldihydrolipoyllysine + CO2
-
?

Synonyms

Synonyms Comment Organism
alpha-ketoglutarate dehydrogenase complex
-
Homo sapiens
alpha-ketoglutarate dehydrogenase complex
-
Bos taurus
KGDHC
-
Homo sapiens
KGDHC
-
Bos taurus

pH Range

pH Minimum pH Maximum Comment Organism
5.7 6
-
Bos taurus