Determination of 17α-hydroxylase-C17,20-lyase (P45017α) enzyme activities and their inhibition by selected steroidal picolyl and picolinylidene compounds

Nikoletta Szabó, Jovana J. Ajdukovic, Evgenija A. Djurendic, Marija N. Sakac, Imre Ignáth, János Gardi, Gábor Mahmoud, Olivera R. Klisuric, Suzana Jovanović-Šanta, Katarina M.Penov Gaši, Mihály Szécsi

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

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 radiosubstrate 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.

Original languageEnglish
Pages (from-to)41-51
Number of pages11
JournalActa biologica Hungarica
Volume66
Issue number1
DOIs
Publication statusPublished - Jan 1 2015

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Keywords

  • 17α-hydroxylase-C
  • Abiraterone
  • Ec 1.14.99.9/ec 4.1.2.30
  • Exo-heterocyclic steroids
  • Lyase (P450) inhibitors
  • Rat testis

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Environmental Science(all)
  • Neurology

Cite this

Szabó, N., Ajdukovic, J. J., Djurendic, E. A., Sakac, M. N., Ignáth, I., Gardi, J., Mahmoud, G., Klisuric, O. R., Jovanović-Šanta, S., Gaši, K. M. P., & Szécsi, M. (2015). Determination of 17α-hydroxylase-C17,20-lyase (P45017α) enzyme activities and their inhibition by selected steroidal picolyl and picolinylidene compounds. Acta biologica Hungarica, 66(1), 41-51. https://doi.org/10.1556/ABiol.66.2015.1.4