20-fluoro-17(20)-pregnenolone derivatives were designed as enol mimics of pregnenolone. All of the targeted, novel fluoroolefins were potent inhibitors of C17(20) lyase.
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How Is CYP17A1 Activity Altered in Autism? A Pilot Study to Identify Potential Pharmacological Targets.
Life (Basel)
June 2022
Teaching Hospital Internal Medicine, Lindenhofgruppe, 3006 Berne, Switzerland.
Increasing evidence exists that higher levels of androgens can be found in individuals with autism. Evidence yields to a susceptible role of Cytochrome P450 17A1 (CYP17A1) with its catalyzation of the two distinct types of substrate oxidation by a hydroxylase activity (17-alpha hydroxylase) and C17/20 lyase activity. However, to what extent steps are altered in affected children with autism versus healthy controls remains to be elucidated.
View Article and Find Full Text PDFInsulin-like growth factors 1 and 2 regulate gene expression and enzymatic activity of in ovarian follicles of the yellowtail, .
Heliyon
June 2020
Seikai National Fisheries Research Institute, Japan Fisheries Research and Education Agency, Taira-machi, Nagasaki 851-2213, Japan.
There is accumulating evidence that insulin-like growth factors (IGFs), primary mediators of somatic growth, play an important role in fish reproduction. Previously, we showed that IGF-1 and IGF-2 are expressed in the ovarian follicle cells of the yellowtail () during the vitellogenic phase, suggesting that IGFs may be involved in ovarian steroidogenesis. In this study, we examined the effects of IGF-1 and IGF-2 on gene expression and activity of steroidogenic enzymes in yellowtail ovary .
View Article and Find Full Text PDFStereochemical investigations of the Tetrahymena cyclase, a model system for euphane/tirucallane biosynthesis.
Org Biomol Chem
March 2017
Department of Chemistry, State University of New York, College of Environmental Science and Forestry, Syracuse, NY 13210, USA.
The squalene cyclase of Tetrahymena pyriformis cyclizes 2,3-dihydrosqualene to euph-7-ene. This was used as a model for euphane biosynthesis. D-ring formation was demonstrated to involve pre-chair folding through an experiment with 2,3-dihydro-5-oxasqualene.
View Article and Find Full Text PDFCharacterization and expression of cDNAs encoding P450c17-II (cyp17a2) in Japanese eel during induced ovarian development.
Gen Comp Endocrinol
September 2015
Division of Marine Life Science, Graduate School of Fisheries Sciences, Hokkaido University, Minato-cho 3-1-1, Hakkodate, Hokkaido 041-8611, Japan. Electronic address:
Article Synopsis
- Estradiol-17β (E2) and maturation-inducing hormone (MIH) are crucial steroid hormones in Japanese eel ovaries, facilitating oocyte maturation and ovulation by shifting hormone production from estrogens to progestogens.
- The study focused on the enzymatic activity of P450c17, particularly the cDNA encoding P450c17-II (cyp17a2), to understand the hormonal transition and reasons for unsuccessful maturation in artificially treated eels.
- Findings revealed five variants of P450c17-II, with evidence of 17α-hydroxylase activity but lacking C17-20 lyase activity; while cyp17a2 showed increased expression during vitellogenesis, c
Molecular pathways: Inhibiting steroid biosynthesis in prostate cancer.
Clin Cancer Res
July 2013
Prostate Cancer Targeted Therapy Group and Drug Development Unit, The Royal Marsden NHS Foundation Trust and The Institute of Cancer Research, Sutton, Surrey, United Kingdom.
A significant proportion of castration-resistant prostate cancers (CRPC) remains driven by ligand activation of the androgen receptor. Although the testes are the primary source of testosterone, testosterone can also be produced from peripheral conversion of adrenal sex hormone precursors DHEA and androstenedione in the prostate and other tissues. CYP17A1 catalyzes two essential reactions in the production of DHEA and androstenedione: the hydroxylation (hydroxylase activity) and the subsequent cleavage of the C17-20 side chain (lyase activity).
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