Determination of 17α-hydroxylase-C17,20-lyase (P45017α) enzyme activities and their inhibition by selected steroidal picolyl and picolinylidene compounds.
17α-hydroxylase-C17,20-lyase (P45017α) is a key regulator enzyme of the steroid hormone biosynthesis in both the adrenals and the testes. Inhibition of this enzyme can block androgen synthesis in an early step, and may thereby be useful in the treatment of several androgen-dependent diseases. We developed radio-substrate in vitro incubation methods for the determination of the distinct 17α-hydroxylase and C17,20-lyase activities of the enzyme using rat testicular homogenate as enzyme source. With this method we have studied the inhibiting activity of selected steroidal picolyl and picolinylidene compounds. Tests revealed a substantial inhibitory action of the 17-picolinyliden-androst-4-en-3-one compound.
University of Szeged 1st Department of Medicine Korányi fasor 8-10 H-6720 Szeged Hungary.
Nikoletta
N
Szabó
University of Novi Sad Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences 3 Trg D. Obradovica 21000 Novi Sad Serbia.
Jovana J
JJ
Ajduković
University of Novi Sad Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences 3 Trg D. Obradovica 21000 Novi Sad Serbia.
Evgenija A
EA
Djurendić
University of Novi Sad Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences 3 Trg D. Obradovica 21000 Novi Sad Serbia.
Marija N
MN
Sakač
University of Szeged 1st Department of Medicine Korányi fasor 8-10 H-6720 Szeged Hungary.
Imre
I
Ignáth
University of Szeged 1st Department of Medicine Korányi fasor 8-10 H-6720 Szeged Hungary.
János
J
Gardi
University of Szeged 1st Department of Medicine Korányi fasor 8-10 H-6720 Szeged Hungary.
Gábor
G
Mahmoud
University of Novi Sad Department of Physics, Faculty of Sciences 4 Trg D. Obradovica 21000 Novi Sad Serbia.
Olivera R
OR
Klisurić
University of Novi Sad Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences 3 Trg D. Obradovica 21000 Novi Sad Serbia.
Suzana
S
Jovanović-Šanta
University of Novi Sad Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences 3 Trg D. Obradovica 21000 Novi Sad Serbia.
Katarina M
KM
Penov Gaši
University of Szeged 1st Department of Medicine Korányi fasor 8-10 H-6720 Szeged Hungary.
Mihály
M
Szécsi
D000818:Animals; D008297:Male; D051381:Rats; D013254:Steroid 17-alpha-Hydroxylase / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013256:Steroids / Q000494:pharmacology*; D013737:Testis / Q000187:drug effects / Q000201:enzymology
D013256:Steroids; D013254:Steroid 17-alpha-Hydroxylase
17α-hydroxylase-C17,20-lyase (P45017α) inhibitors; EC 1.14.99.9 / EC 4.1.2.30; abiraterone; exo-heterocyclic steroids; rat testis