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Literature summary extracted from

  • Rahaman, M.M.; Reinders, F.G.; Koes, D.; Nguyen, A.T.; Mutchler, S.M.; Sparacino-Watkins, C.; Alvarez, R.A.; Miller, M.P.; Cheng, D.; Chen, B.B.; Jackson, E.K.; Camacho, C.J.; Straub, A.C.
    Structure guided chemical modifications of propylthiouracil reveal novel small molecule inhibitors of cytochrome b5 reductase 3 that increase nitric oxide bioavailability (2015), J. Biol. Chem., 290, 16861-16872 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.6.2.2 expressed in Escherichia coli SoluBL21 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.6.2.2 (5Z)-5-[(9H-fluoren-3-yl)methylidene]-1-(4-methylphenyl)-2-sulfanylidenedihydropyrimidine-4,6(1H,5H)-dione about 80% inhibition at 0.5 mM Homo sapiens
1.6.2.2 (5Z)-5-{[4-bromo-5-(morpholin-4-yl)furan-2-yl]methylidene}-1-(4-methylphenyl)-2-sulfanylidenedihydropyrimidine-4,6(1H,5H)-dione about 5% inhibition at 0.5 mM Homo sapiens
1.6.2.2 1-(2-fluorophenyl)-5-[(1-methyl-2,3-dihydro-1H-indol-3-yl)methyl]-2-sulfanylidenedihydropyrimidine-4,6(1H,5H)-dione about 75% inhibition at 0.5 mM Homo sapiens
1.6.2.2 2-methyl-6-[(phenylsulfanyl)methyl]-2,5-dihydropyrimidin-4(3H)-one about 5% inhibition at 0.5 mM Homo sapiens
1.6.2.2 4-({[(2S)-2,3-dihydro-1,3-benzoxazol-2-yl]sulfanyl}methyl)tetrahydropyrimidine-2,5-dione about 45% inhibition at 0.5 mM Homo sapiens
1.6.2.2 5-(prop-2-en-1-yl)-6-propyl-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 75% inhibition at 0.5 mM Homo sapiens
1.6.2.2 6-(pentyloxy)-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 25% inhibition at 0.05 mM Homo sapiens
1.6.2.2 6-([[(2R)-2,3-dihydro-1,3-benzoxazol-2-yl]sulfanyl]methyl)-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one complete inhibition at 0.05 mM Homo sapiens
1.6.2.2 6-benzyl-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 3% inhibition at 0.5 mM Homo sapiens
1.6.2.2 6-pentyl-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 25% inhibition at 0.5 mM Homo sapiens
1.6.2.2 6-[(phenylsulfanyl)methyl]-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one complete inhibition at 0.05 mM Homo sapiens
1.6.2.2 6-[(phenylsulfanyl)methyl]pyrimidine-2,4(1H,3H)-dione about 50% inhibition at 0.5 mM Homo sapiens
1.6.2.2 6-{[(2,6-dichlorophenyl)sulfanyl]methyl}-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one complete inhibition at 0.05 mM Homo sapiens
1.6.2.2 6-{[(4-bromophenyl)sulfanyl]methyl}-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 10% inhibition at 0.05 mM Homo sapiens
1.6.2.2 6-{[(4-methylphenyl)sulfanyl]methyl}-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 85% inhibition at 0.05 mM Homo sapiens
1.6.2.2 6-{[(propan-2-yl)sulfanyl]methyl}-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 18% inhibition at 0.05 mM Homo sapiens
1.6.2.2 propylthiouracil complete inhibition at 0.5 mM Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.6.2.2 NADH + ferricytochrome b5 Homo sapiens
-
 NAD+ + H+ + ferrocytochrome b5
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.6.2.2 Homo sapiens P00387
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.6.2.2 Ni-NTA column chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.6.2.2 NADH + ferricyanide
-
 Homo sapiens NAD+ + H+ + ferrocyanide
-
 ?
1.6.2.2 NADH + ferricytochrome b5
-
 Homo sapiens NAD+ + H+ + ferrocytochrome b5
-
 ?

Subunits

EC Number Subunits Comment Organism
1.6.2.2 ? x * 34000, SDS-PAGE Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
1.6.2.2 CYB5R3
-
 Homo sapiens
1.6.2.2 cytochrome b5 reductase 3
-
 Homo sapiens
1.6.2.2 methemoglobin reductase
-
 Homo sapiens
1.6.2.2 NADH: ferricytochrome b5 oxidoreductase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.6.2.2 FAD
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.6.2.2 0.00914
-
 at pH 7.5 and 37°C Homo sapiens 6-([[(2R)-2,3-dihydro-1,3-benzoxazol-2-yl]sulfanyl]methyl)-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one
1.6.2.2 0.0108
-
 at pH 7.5 and 37°C Homo sapiens 6-[(phenylsulfanyl)methyl]-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one
1.6.2.2 0.2794
-
 at pH 7.5 and 37°C Homo sapiens propylthiouracil

General Information

EC Number General Information Comment Organism
1.6.2.2 physiological function the enzyme regulates nitric oxide diffusion in the artery wall Homo sapiens