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Literature summary extracted from

  • Mbenza, N.M.; Nasarudin, N.; Vadakkedath, P.G.; Patel, K.; Ismail, A.Z.; Hanif, M.; Wright, L.J.; Sarojini, V.; Hartinger, C.G.; Leung, I.K.H.
    Carbon monoxide is an inhibitor of HIF prolyl hydroxylase domain 2 (2021), ChemBioChem, 22, 2521-2525 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.11.29 CO releasing molecule-2 i.e.CORM-2, [RuCl2(CO)3]2, in situ CO donor, reduces the hydroxylation of C-terminal and N-terminal oxygen-dependent degradation domains of HIF-1alpha Homo sapiens
1.14.11.29 RuCl3 inhibitor of PHD2 under the standard assay conditions in presence of 10 microM Fe(II). This effect can be alleviated by supplementing the enzymatic reaction mixture with excess Fe(II) Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.14.11.29 0.0052
-
 DLDLEMLAPYIPMDDDFQL pH 7.5, 37°C Homo sapiens
1.14.11.29 0.0366
-
 DALTLLAPAAGDTIISLDF pH 7.5, 37°C Homo sapiens
1.14.11.29 0.1071
-
 DALTLLAPAAGDTIISLDF pH 7.5, 37°C Homo sapiens
1.14.11.29 0.1306
-
 DLDLEMLAPYIPTIISLDF pH 7.5, 37°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.14.11.29 Homo sapiens Q9GZT9
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.11.29 DALTLLAPAAGDTIISLDF + 2-oxoglutarate + O2 hybrid substrate derived from C-terminal and N-terminal oxygen-dependent degradation domain Homo sapiens DALTLLA-((4R)-4-hydroxy-L-proline)-AAGDTIISLDF + succinate + CO2
-
 ?
1.14.11.29 DALTLLAPAAGDTIISLDF + 2-oxoglutarate + O2 substrate derived from N-terminal oxygen-dependent degradation domain Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-AAGDTIISLDF + succinate + CO2
-
 ?
1.14.11.29 DLDLEMLAPYIPMDDDFQL + 2-oxoglutarate + O2 substrate derived from C-terminal oxygen-dependent degradation domain Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-YIPMDDDFQL + succinate + CO2
-
 ?
1.14.11.29 DLDLEMLAPYIPTIISLDF + 2-oxoglutarate + O2 hybrid substrate derived from C-terminal and N-terminal oxygen-dependent degradation domain Homo sapiens DLDLEMLA-((4R)-4-hydroxy-L-proline)-YIPTIISLDF + succinate + CO2
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.14.11.29 0.0244
-
 substrate DLDLEMLAPYIPTIISLDF, pH 7.5, 37°C Homo sapiens CO releasing molecule-2
1.14.11.29 0.0342
-
 substrate DALTLLAPAAGDTIISLDF, pH 7.5, 37°C Homo sapiens CO releasing molecule-2
1.14.11.29 0.0468
-
 substrate DALTLLAPAAGDTIISLDF, pH 7.5, 37°C Homo sapiens CO releasing molecule-2
1.14.11.29 0.1425
-
 substrate DLDLEMLAPYIPMDDDFQL, pH 7.5, 37°C Homo sapiens CO releasing molecule-2