Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Perchellet, J.P.; Perchellet, E.M.; Crow, K.R.; Buszek, K.R.; Brown, N.; Ellappan, S.; Gao, G.; Luo, D.; Minatoya, M.; Lushington, G.H.
    Novel synthetic inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity that inhibit tumor cell proliferation and are structurally unrelated to existing statins (2009), Int. J. Mol. Med., 24, 633-643.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.34 fluvastatin
-
 Homo sapiens
1.1.1.34 lovastatin
-
 Homo sapiens
1.1.1.34 mevastatin
-
 Homo sapiens
1.1.1.34 additional information screening of eight-membered medium ring lactams and related tricyclic compounds, either seven-membered lactams, thiolactams or amines, for inhibitory potency, overview. The compounds are inhibitory also in the presence of increasing concentrations of NADPH, and are not affected by increasing concentrations of HMG-CoA. Medium ring lactams and existing statins may have different mechanisms of enzyme interaction and inhibition, molecular docking studies and comparisons using the HMG-CoA reductase statin-binding receptor model, overview. The ligands may occupy a narrow channel housing the pyridinium moiety on NADP+ Homo sapiens
1.1.1.34 pravastatin inhibitory in the presence of increasing concentrations of NADPH, but increasing concentrations of HMG-CoA block the HMG-CoA reductase-inhibiting activity Homo sapiens
1.1.1.34 simvastatin
-
 Homo sapiens
1.1.1.88 (3S,6Z)-3-benzyl-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-4-(3-methylbutanoyl)-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one purified enzyme, 52.6% residual activity at 0.01 mM Homo sapiens
1.1.1.88 (3S,6Z)-3-benzyl-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-4-(3-methylbutanoyl)-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one antiproliferative activity in L-1210 cell, IC50 0.00148 mM Mus musculus
1.1.1.88 (3S,6Z)-3-benzyl-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-4-[[(E)-2-phenylethenyl]sulfonyl]-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one purified enzyme, 32.3% residual activity at 0.01 mM Homo sapiens
1.1.1.88 (3S,6Z)-3-benzyl-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-4-[[(E)-2-phenylethenyl]sulfonyl]-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one antiproliferative activity in L-1210 cell, IC50 0.0023 mM Mus musculus
1.1.1.88 (3S,6Z)-3-benzyl-4-(3,3-dimethylbutanoyl)-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one purified enzyme, 43.4% residual activity at 0.01 mM Homo sapiens
1.1.1.88 (3S,6Z)-3-benzyl-4-(3,3-dimethylbutanoyl)-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one antiproliferative activity in L-1210 cell, IC50 0.00143 mM Mus musculus
1.1.1.88 (3S,6Z)-4-(biphenyl-4-ylsulfonyl)-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-3-methyl-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one purified enzyme, 54.4% residual activity at 0.01 mM Homo sapiens
1.1.1.88 (3S,6Z)-4-(biphenyl-4-ylsulfonyl)-1-(4-fluorobenzyl)-8-(4-methoxyphenyl)-3-methyl-3,4,5,8-tetrahydro-1,4-diazocin-2(1H)-one antiproliferative activity in L-1210 cell, IC50 0.00119 mM Mus musculus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.34 3-hydroxy-3-methylglutaryl-CoA + 2 NADPH + 2 H+ Homo sapiens
-
 mevalonate + CoA + 2 NADP+
-
 r

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.34 Homo sapiens P04035
-
-
1.1.1.88 Homo sapiens
-
-
-
1.1.1.88 Mus musculus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.88
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.88 L-1210 cell
-
 Mus musculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.34 3-hydroxy-3-methylglutaryl-CoA + 2 NADPH + 2 H+
-
 Homo sapiens mevalonate + CoA + 2 NADP+
-
 r

Synonyms

EC Number Synonyms Comment Organism
1.1.1.34 3-hydroxy-3-methylglutaryl-coenzyme A reductase
-
 Homo sapiens
1.1.1.34 HMG-CoA reductase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.34 NADP+
-
 Homo sapiens
1.1.1.34 NADPH
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
1.1.1.34 metabolism HMG-CoA reductase is the rate-limiting enzyme of cholesterol biosynthesis Homo sapiens