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Literature summary extracted from

  • McNaught, K.S.; Altomare, C.; Cellamare, S.; Carotti, A.; Thull, U.; Carrupt, P.A.; Testa, B.; Jenner, P.; Marsden, C.D.
    Inhibition of alpha-ketoglutarate dehydrogenase by isoquinoline derivatives structurally related to 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) (1995), NeuroReport, 6, 1105-1108.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.2.1.105 1,2,3,4-tetrahydroisoquinoline IC50: 18.2 Rattus norvegicus
1.2.1.105 1-methyl-4-phenylpyridinium IC50: 18.9 mM Rattus norvegicus
1.2.1.105 Isoquinoline IC50: 6.5 mM Rattus norvegicus
1.2.1.105 N-methyl-1,2,3,4-tetrahydroisoquinoline IC50: 2 mM Rattus norvegicus
1.2.1.105 N-methylisoquinolinium
-
 Rattus norvegicus
1.2.1.105 N-n-propylisoquinolinium IC50: 3 mM Rattus norvegicus
1.2.1.105 salsolinol
-
 Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.2.1.105 mitochondrion
-
 Rattus norvegicus 5739
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.2.1.105 2-oxoglutarate + lipoamide Rattus norvegicus catalyzes a rate limiting step of the TCA cycle S-succinyldihydrolipoamide + CO2
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.2.1.105 Rattus norvegicus
-
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
1.2.1.105 2-oxoglutarate + [dihydrolipoyllysine-residue succinyltransferase] lipoyllysine = [dihydrolipoyllysine-residue succinyltransferase] S-succinyldihydrolipoyllysine + CO2 the enzyme complex catalyzes the reaction : 2-oxoglutarate + CoA + NAD+--> succinyl-CoA + CO2 + NADH, the following partial reactions are catalyzed: 1. HOOC(CH2)2COCOOH + (thiamine diphosphate)-E1--> (HOOC(CH2)2 CHOH-thiamine-diphosphate)-E1 + CO2, 2. (HOOC(CH2)2CH OH-thiamine-diphosphate)-E1 + (LipS2)-E2--> (HOOC(CH)2 CO-(SLipSH))-E2 + (thiamine-diphosphate)-E1, 3. (HOOC(CH2)2CO-(SLipSH))-E2 + HSCoA--> (Lip(SH)2)-E2 + HOOC(CH2)2CO-SCoA, 4. (Lip(SH)2)-E2 + E3-FAD--> (LipS2)-E2 + reduced E3-FAD, 5. reduced E3-FAD + NAD+--> E3-FAD + NADH Rattus norvegicus
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.2.1.105 brain forebrain Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.2.1.105 2-oxoglutarate + lipoamide
-
 Rattus norvegicus S-succinyldihydrolipoamide + CO2
-
 ?
1.2.1.105 2-oxoglutarate + lipoamide catalyzes a rate limiting step of the TCA cycle Rattus norvegicus S-succinyldihydrolipoamide + CO2
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.2.1.105 2
-
 IC50: 2 mM Rattus norvegicus N-methyl-1,2,3,4-tetrahydroisoquinoline
1.2.1.105 3
-
 IC50: 3 mM Rattus norvegicus N-n-propylisoquinolinium
1.2.1.105 6.5
-
 IC50: 6.5 mM Rattus norvegicus Isoquinoline
1.2.1.105 18.2
-
 IC50: 18.2 mM Rattus norvegicus 1,2,3,4-tetrahydroisoquinoline
1.2.1.105 18.9
-
 IC50: 18.9 mM Rattus norvegicus 1-methyl-4-phenylpyridinium