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Literature summary for 1.6.2.2 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
Search for more literature for 1.6.2.2

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
(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
(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-(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
2-methyl-6-[(phenylsulfanyl)methyl]-2,5-dihydropyrimidin-4(3H)-one about 5% inhibition at 0.5 mM Homo sapiens
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
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
6-(pentyloxy)-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 25% inhibition at 0.05 mM Homo sapiens
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
6-benzyl-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 3% inhibition at 0.5 mM Homo sapiens
6-pentyl-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 25% inhibition at 0.5 mM Homo sapiens
6-[(phenylsulfanyl)methyl]-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one complete inhibition at 0.05 mM Homo sapiens
6-[(phenylsulfanyl)methyl]pyrimidine-2,4(1H,3H)-dione about 50% inhibition at 0.5 mM Homo sapiens
6-{[(2,6-dichlorophenyl)sulfanyl]methyl}-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one complete inhibition at 0.05 mM Homo sapiens
6-{[(4-bromophenyl)sulfanyl]methyl}-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 10% inhibition at 0.05 mM Homo sapiens
6-{[(4-methylphenyl)sulfanyl]methyl}-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 85% inhibition at 0.05 mM Homo sapiens
6-{[(propan-2-yl)sulfanyl]methyl}-2-sulfanylidene-2,3-dihydropyrimidin-4(1H)-one about 18% inhibition at 0.05 mM Homo sapiens
propylthiouracil complete inhibition at 0.5 mM Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P00387
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Subunits

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
FAD
-
 Homo sapiens

IC50 Value

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

General Information

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