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Literature summary for 1.14.14.19 extracted from

  • Kostin, V.A.; Zolottsev, V.A.; Kuzikov, A.V.; Masamrekh, R.A.; Shumyantseva, V.V.; Veselovsky, A.V.; Stulov, S.V.; Novikov, R.A.; Timofeev, V.P.; Misharin, A.Y.
    Oxazolinyl derivatives of [17(20)E]-21-norpregnene differing in the structure of A and B rings. Facile synthesis and inhibition of CYP17A1 catalytic activity (2016), Steroids, 115, 114-122 .
    View publication on PubMed

Application

Application Comment Organism
analysis assay based on direct electrochemistry of CYP17A1 entrapped in didodecyldimethyl ammonium bromide-modified electrode under aerobic conditions in the supporting electrolyte solution Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
molecular docking of inhibitors to the active site Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2'-[[(E)-3-oxoandrost-4-en-17-ylidene]methyl]-4',5'-dihydro-1',3'-oxazole 1 microM, 54% inhibition Homo sapiens
2'-[[(E)-3beta-hydroxyandrost-5-en-17-ylidene]methyl]-4',5'-dihydro-1',3'-oxazole 1 microM, 78% inhibition Homo sapiens
2'-[[(E)-6-oxo-3alpha,5alpha-cycloandrostan-17-ylidene]methyl]-4',5'-dihydro-1',3'-oxazole compound strongly depresses electrocatalytic activity of CYP17A1 toward pregnenolone at concentrations of 0.1 microM and 1 microM, but data do not obey the Michaelis-Menten catalytic model Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P05093
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
pregnenolone + AH2 + O2
-
Homo sapiens 17alpha-hydroxypregnenolone + A + H2O
-
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