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Literature summary for 1.2.1.105 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

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

Localization

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Reaction

Reaction Comment Organism Reaction ID
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

Source Tissue

Source Tissue Comment Organism Textmining
brain forebrain Rattus norvegicus
-

Substrates and Products (Substrate)

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

IC50 Value

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