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Literature summary for 1.14.11.29 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
Search for more literature for 1.14.11.29

Inhibitors

Inhibitors Comment Organism Structure
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
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]

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

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9GZT9
-
-

Substrates and Products (Substrate)

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

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