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Literature summary for 4.6.1.2 extracted from

  • Lamothe, M.; Chang, F.J.; Balashova, N.; Shirokov, R.; Beuve, A.
    Functional Characterization of Nitric Oxide and YC-1 Activation of Soluble Guanylyl Cyclase: Structural Implication for the YC-1 Binding Site? (2004), Biochemistry, 43, 3039-3048.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
1-benzyl-3-(hydroxymethyl-2-furyl)indazole trivial name YC-1, allosteric activator, synergistically increases the catalytic activity in the presence of NO Rattus norvegicus
N-(beta-D-glucopyranosyl-N2-acetyl-S-nitroso-D,L-penicillaminamide) NO donor Rattus norvegicus
NO binds at beta1 subunit heme, several hundred fold increase in activity Rattus norvegicus
sodium nitroprusside NO donor Rattus norvegicus

Cloned(Commentary)

Cloned (Comment) Organism
expression of sGC in Sf9 insect cells and COS-7 cells Rattus norvegicus

Protein Variants

Protein Variants Comment Organism
C238S no change in cGMP production Rattus norvegicus
C243S no change in cGMP production Rattus norvegicus
C594D no 1-benzyl-3-(hydroxymethyl-2-furyl)indazole activation, no synergy with NO Rattus norvegicus
C594D/E525K loss of activity Rattus norvegicus
C594Y reduced level of NO and 1-benzyl-3-(hydroxymethyl-2-furyl)indazole activation Rattus norvegicus
D477A reduced level of NO and 1-benzyl-3-(hydroxymethyl-2-furyl)indazole activation Rattus norvegicus
M537N high level of 1-benzyl-3-(hydroxymethyl-2-furyl)indazole activation Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.025
-
GTP 30°C, pH 8.0, in the presence of N-(beta-D-glucopyranosyl-N2-acetyl-S-nitroso-D,L-penicillaminamide) and YC-1 Rattus norvegicus
0.039
-
GTP 30°C, pH 8.0, in the presence of YC-1 Rattus norvegicus
0.061
-
GTP 30°C, pH 8.0, in the presence of N-(beta-D-glucopyranosyl-N2-acetyl-S-nitroso-D,L-peniciiaminamide) Rattus norvegicus
0.12
-
GTP 30°C, pH 8.0, basal activity Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
GTP Rattus norvegicus
-
3',5'-cyclic GMP + diphosphate
-
?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant sGC Rattus norvegicus

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.12
-
basal activity Rattus norvegicus
9.1
-
in the presence of 0.1 mM N-(beta-D-glucopyranosyl-N2-acetyl-S-nitroso-D,L-penicillaminamide) Rattus norvegicus
12.1
-
in the presence of 0.1 mM N-(beta-D-glucopyranosyl-N2-acetyl-S-nitroso-D,L-penicillaminamide) and YC-1 Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP
-
Rattus norvegicus 3',5'-cyclic GMP + diphosphate
-
?

Synonyms

Synonyms Comment Organism
sGC
-
Rattus norvegicus
soluble guanylyl cyclase
-
Rattus norvegicus