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Literature summary extracted from

  • Pallan, P.S.; Nagy, L.D.; Lei, L.; Gonzalez, E.; Kramlinger, V.M.; Azumaya, C.M.; Wawrzak, Z.; Waterman, M.R.; Guengerich, F.P.; Egli, M.
    Structural and kinetic basis of steroid 17?,20-lyase activity in teleost fish cytochrome P450 17A1 and its absence in cytochrome P450 17A2 (2015), J. Biol. Chem., 290, 3248-3268.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.14.14.19 expressed in Escherichia coli BL21-Gold (DE3) cells Danio rerio

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.14.14.19 isoform P450 17A1 in complex with either abiraterone or progesterone, sitting drop vapor diffusion method, using 100 mM sodium HEPES buffer (pH 7.5), 50 mM MgCl2, and 20-30% (w/v) polyethylene glycol monomethyl ether 3550 Danio rerio
1.14.14.19 isoform P450 17A2 in complex with either abiraterone or progesterone, sitting drop vapor diffusion method, using 100 mM sodium HEPES buffer (pH 7.5), 50 mM MgCl2, and 20-30% (w/v) polyethylene glycol monomethyl ether 3550 Danio rerio

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.14.19 abiraterone
-
 Danio rerio
1.14.14.19 orteronel
-
 Danio rerio

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.14.14.19 0.0017
-
 progesterone isoform P450 17A1, at pH 7.4 and 37°C Danio rerio
1.14.14.19 0.002
-
 pregnenolone isoform P450 17A1, at pH 7.4 and 37°C Danio rerio
1.14.14.19 0.0093
-
 pregnenolone isoform P450 17A2, at pH 7.4 and 37°C Danio rerio
1.14.14.19 0.03
-
 progesterone isoform P450 17A2, at pH 7.4 and 37°C Danio rerio

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
1.14.14.19 51500
-
 x * 51500, isoform P450 17A1, calculated from amino acid sequence Danio rerio
1.14.14.19 54000
-
 x * 54000, isoform P450 17A2, calculated from amino acid sequence Danio rerio

Organism

EC Number Organism UniProt Comment Textmining
1.14.14.19 Danio rerio A7U483
-
-
1.14.14.19 Danio rerio B3DH80
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.14.14.19 Ni-NTA column chromatography, DEAE column chromatography, and SP-Sepharose column chromatography Danio rerio

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.14.19 additional information isoform P450 17A1 also exhibits 17alpha,20-lyase activity Danio rerio ?
-
 ?
1.14.14.19 pregnenolone + [reduced NADPH-hemoprotein reductase] + O2
-
 Danio rerio 17alpha-hydroxypregnenolone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
1.14.14.19 progesterone + [reduced NADPH-hemoprotein reductase] + O2
-
 Danio rerio 17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
1.14.14.19 progesterone + [reduced NADPH-hemoprotein reductase] + O2 isoform P450 17A1 has 3fold higher catalytic efficiency in the 17alpha-hydroxylation of progesterone than pregnenolone Danio rerio 17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?

Subunits

EC Number Subunits Comment Organism
1.14.14.19 ? x * 51500, isoform P450 17A1, calculated from amino acid sequence Danio rerio
1.14.14.19 ? x * 54000, isoform P450 17A2, calculated from amino acid sequence Danio rerio

Synonyms

EC Number Synonyms Comment Organism
1.14.14.19 cytochrome P450 17A1
-
 Danio rerio
1.14.14.19 cytochrome P450 17A2
-
 Danio rerio

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.14.14.19 0.03
-
 pregnenolone isoform P450 17A1, at pH 7.4 and 37°C Danio rerio
1.14.14.19 0.1
-
 progesterone isoform P450 17A1, at pH 7.4 and 37°C Danio rerio
1.14.14.19 0.85
-
 pregnenolone isoform P450 17A2, at pH 7.4 and 37°C Danio rerio
1.14.14.19 1.6
-
 progesterone isoform P450 17A2, at pH 7.4 and 37°C Danio rerio

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.14.14.19 0.00000035
-
 isoform P450 17A1, with pregnenolone as substrate, at pH 7.4b and 37°C Danio rerio orteronel
1.14.14.19 0.0000011
-
 isoform P450 17A2, with progesterone as substrate, at pH 7.4b and 37°C Danio rerio orteronel
1.14.14.19 0.000015
-
 isoform P450 17A1, with progesterone as substrate, at pH 7.4b and 37°C Danio rerio orteronel
1.14.14.19 0.00079
-
 isoform P450 17A2, with pregnenolone as substrate, at pH 7.4b and 37°C Danio rerio orteronel

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
1.14.14.19 16.7
-
 pregnenolone isoform P450 17A1, at pH 7.4 and 37°C Danio rerio
1.14.14.19 53.3
-
 progesterone isoform P450 17A2, at pH 7.4 and 37°C Danio rerio
1.14.14.19 56.7
-
 progesterone isoform P450 17A1, at pH 7.4 and 37°C Danio rerio
1.14.14.19 91.7
-
 pregnenolone isoform P450 17A2, at pH 7.4 and 37°C Danio rerio