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Literature summary for 1.14.19.20 extracted from

  • Giera, M.; Renard, D.; Ploessl, F.; Bracher, F.
    Lathosterol side chain amides—a new class of human lathosterol oxidase inhibitors (2008), Steroids, 73, 299-308.
    View publication on PubMed
Search for more literature for 1.14.19.20

Inhibitors

Inhibitors Comment Organism Structure
(3S,20S)-20-N-(2-methylpropyl)carbamoylpregn-7-en-3beta-ol specific Homo sapiens
(3S,20S)-20-N-(2-methylpropyl)carbamoylpregn-7-en-3beta-yl acetate specific for the enzyme. Prodrug, transformed into the 3beta-hydroxy derivative under in vitro conditions Homo sapiens
(3S,20S)-20-N-butylcarbamoylpregn-7-en-3beta-ol specific Homo sapiens
(3S,20S)-20-N-butylcarbamoylpregn-7-en-3beta-yl acetate specific for the enzyme. Prodrug, transformed into the 3beta-hydroxy derivative under in vitro conditions Homo sapiens
(3S,20S)-20-N-ethylcarbamoylpregn-7-en-3beta-ol
-
 Homo sapiens
(3S,20S)-20-N-ethylcarbamoylpregn-7-en-3beta-yl acetate
-
 Homo sapiens
(3S,20S)-20-N-pentylcarbamoylpregn-7-en-3beta-ol specific Homo sapiens
(3S,20S)-20-N-pentylcarbamoylpregn-7-en-3beta-yl acetate specific for the enzyme. Prodrug, transformed into the 3beta-hydroxy derivative under in vitro conditions Homo sapiens
(3S,20S)-20-N-propylcarbamoylpregn-7-en-3beta-ol
-
 Homo sapiens
(3S,20S)-20-N-propylcarbamoylpregn-7-en-3beta-yl acetate
-
 Homo sapiens
(3S,20S)-20-N-tert-butylcarbamoylpregn-7-en-3beta-ol specific Homo sapiens
(3S,20S)-20-N-tert-butylcarbamoylpregn-7-en-3beta-yl acetate specific for the enzyme. Prodrug, transformed into the 3beta-hydroxy derivative under in vitro conditions Homo sapiens
lathosterol side chain amides synthesis and compound screening, influence of different sterol amides on inhibition of the enzyme, overview, lathosterol-derived amides with larger substituents, e.g. butyl, isobutyl, tert-butyl, pentyl, at the amide nitrogen are selective inhibitors of lathosterol oxidase, overview Homo sapiens
additional information cytotoxicity and inhibitor potencies for inhibition of total cholesterol biosynthesis, overview Homo sapiens
Triarimol weak inhibition Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane bound Homo sapiens 16020
-
microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens the enzyme is involved in the post-squalene part of cholesterol biosynthesis ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HL-60 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the enzyme is involved in the post-squalene part of cholesterol biosynthesis Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
5-DES
-
 Homo sapiens
DELTA7-sterol-C5(6)-desaturase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00033
-
 inhibition of total cholesterol production Homo sapiens (3S,20S)-20-N-(2-methylpropyl)carbamoylpregn-7-en-3beta-ol
0.00045
-
 inhibition of total cholesterol production Homo sapiens (3S,20S)-20-N-(2-methylpropyl)carbamoylpregn-7-en-3beta-yl acetate
0.0007
-
 inhibition of total cholesterol production Homo sapiens (3S,20S)-20-N-butylcarbamoylpregn-7-en-3beta-ol
0.00091
-
 inhibition of total cholesterol production Homo sapiens (3S,20S)-20-N-butylcarbamoylpregn-7-en-3beta-yl acetate
0.00095
-
 inhibition of total cholesterol production Homo sapiens (3S,20S)-20-N-tert-butylcarbamoylpregn-7-en-3beta-yl acetate
0.00105
-
 inhibition of total cholesterol production Homo sapiens (3S,20S)-20-N-tert-butylcarbamoylpregn-7-en-3beta-ol
0.0011
-
 inhibition of total cholesterol production Homo sapiens (3S,20S)-20-N-pentylcarbamoylpregn-7-en-3beta-yl acetate
0.00116
-
 inhibition of total cholesterol production Homo sapiens (3S,20S)-20-N-pentylcarbamoylpregn-7-en-3beta-ol