DETERMINATION OF 17α-HYDROXYLASE-C17,20-LYASE (P45017α) ENZYME ACTIVITIES AND THEIR INHIBITION BY SELECTED STEROIDAL PICOLYL AND PICOLINYLIDENE COMPOUNDS

被引：19
作者：
Szabo, Nikoletta [1 ]
Ajdukovic, Jovana J. [2 ]
Djurendic, Evgenija A. [2 ]
Sakac, Marija N. [2 ]
Ignath, Imre [1 ]
Gardi, Janos [1 ]
Mahmoud, Gabor [1 ]
Klisuric, Olivera R. [3 ]
Jovanovic-Santa, Suzana [2 ]
Gasi, Katarina M. Penov [2 ]
Szecsi, Mihaly [1 ]
机构：
[1] Univ Szeged, Dept Med 1, H-6720 Szeged, Hungary
[2] Univ Novi Sad, Fac Sci, Dept Chem Biochem & Environm Protect, Novi Sad 21000, Serbia
[3] Univ Novi Sad, Fac Sci, Dept Phys, Novi Sad 21000, Serbia
来源：
ACTA BIOLOGICA HUNGARICA | 2015年 / 66卷 / 01期
关键词：
EC; 1.14.99.9; /; 4.1.2.30; 17; alpha-hydroxylase-C-17; C-20-lyase; (P450(17; alpha)); inhibitors; exo-heterocyclic steroids; rat testis; abiraterone; HUMAN CYTOCHROME P450(17-ALPHA); PROSTATE-CANCER; ABIRATERONE ACETATE; POTENT INHIBITORS; IN-VITRO; DERIVATIVES; CYP17; 17,20-LYASE; 17-PICOLYL; STEROIDOGENESIS;
D O I：
10.1556/ABiol.66.2015.1.4
中图分类号：
Q [生物科学];
学科分类号：
07 ; 0710 ; 09 ;
摘要：
17 alpha-hydroxylase-C-17,C-20-lyase (P450(17 alpha)) 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 radiosubstrate in vitro incubation methods for the determination of the distinct 17 alpha-hydroxylase and C-17,C-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.
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收藏
页码：41 / 51
页数：11
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