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Literature summary for 1.14.14.19 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
Search for more literature for 1.14.14.19

Cloned(Commentary)

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

Crystallization (Commentary)

Crystallization (Comment) Organism
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
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

Inhibitors Comment Organism Structure
abiraterone
-
 Danio rerio
orteronel
-
 Danio rerio

KM Value [mM]

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

Molecular Weight [Da]

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

Organism

Organism UniProt Comment Textmining
Danio rerio A7U483
-
-
Danio rerio B3DH80
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information isoform P450 17A1 also exhibits 17alpha,20-lyase activity Danio rerio ?
-
 ?
pregnenolone + [reduced NADPH-hemoprotein reductase] + O2
-
 Danio rerio 17alpha-hydroxypregnenolone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
progesterone + [reduced NADPH-hemoprotein reductase] + O2
-
 Danio rerio 17alpha-hydroxyprogesterone + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
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

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

Synonyms

Synonyms Comment Organism
cytochrome P450 17A1
-
 Danio rerio
cytochrome P450 17A2
-
 Danio rerio

Turnover Number [1/s]

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

IC50 Value

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

kcat/KM [mM/s]

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