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Agonistic and Antagonistic Effects of Progesterone Derivatives on the Transcriptional Activity of Nuclear Progesterone Receptor B in Yeast Model System.

التفاصيل البيبلوغرافية
العنوان: Agonistic and Antagonistic Effects of Progesterone Derivatives on the Transcriptional Activity of Nuclear Progesterone Receptor B in Yeast Model System.
المؤلفون: Michurina AO; Lomonosov Moscow State University, Faculty of Biology, Moscow, 119899, Russia., Polikarpova AV; Lomonosov Moscow State University, Faculty of Biology, Moscow, 119899, Russia., Levina IS; Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow, 117913, Russia., Kulikova LE; Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow, 117913, Russia., Zavarzin IV; Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Moscow, 117913, Russia., Guseva AA; Lomonosov Moscow State University, Faculty of Biology, Moscow, 119899, Russia., Morozov IA; Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, 119991, Russia., Rubtsov PM; Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, 119991, Russia., Smirnova OV; Lomonosov Moscow State University, Faculty of Biology, Moscow, 119899, Russia., Shchelkunova TA; Lomonosov Moscow State University, Faculty of Biology, Moscow, 119899, Russia. schelkunova-t@mail.ru.
المصدر: Biochemistry. Biokhimiia [Biochemistry (Mosc)] 2018 May; Vol. 83 (5), pp. 574-585.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: MAIK Nauka/Interperiodica Country of Publication: United States NLM ID: 0376536 Publication Model: Print Cited Medium: Internet ISSN: 1608-3040 (Electronic) Linking ISSN: 00062979 NLM ISO Abbreviation: Biochemistry (Mosc) Subsets: MEDLINE
أسماء مطبوعة: Publication: <2007->: Moscow : MAIK Nauka/Interperiodica
Original Publication: New York, Consultants Bureau [etc.]
مواضيع طبية MeSH: Cell Nucleus/*drug effects , Progesterone/*pharmacology , Receptors, Progesterone/*agonists , Receptors, Progesterone/*antagonists & inhibitors , Saccharomyces cerevisiae/*drug effects , Saccharomyces cerevisiae/*genetics , Transcription, Genetic/*drug effects , Transcriptional Activation/*drug effects, Cell Nucleus/metabolism ; Models, Biological ; Progesterone/analogs & derivatives ; Progesterone/chemistry ; Receptors, Progesterone/genetics ; Saccharomyces cerevisiae/cytology ; Saccharomyces cerevisiae/metabolism ; Transcription, Genetic/genetics ; Transcriptional Activation/genetics
مستخلص: Identification of progesterone selective agonists and antagonists that act through one of the nuclear progesterone receptor isoforms is of particular importance for the development of tissue-specific drugs in gynecology and anticancer therapy. Fourteen pregna-D' 6 - and pregna-D' 3 -pentarane progesterone derivatives with 16α,17α-cycloalkane groups and two progesterone 3-deoxyderivatives were examined for their ability to regulate transcriptional activity of human nuclear progesterone receptor isoform B (nPR-B) expressed in Saccharomyces cerevisiae yeast. Transcriptional activity of nPR-B was measured from the expression of the β-galactosidase reporter gene with a hormone-responsible element in the promoter. Among the compounds tested, two were full progesterone agonists, four were partial agonists, one compound possessed both agonistic and antagonistic activity, one compound displayed only partial antagonistic activity, and eight compounds did not show any activity. Modifications of the pentarane structure, precisely, introduction of an additional double bound in the A or B rings and/or modification at the 6th position of progesterone, lead to a switch from the complete agonistic activity to partial agonistic or mixed activities. These modifications enable progestins to act as selective modulators of progesterone receptor. Steroids with reduced A-ring and 3-ketogroups lose their ability to regulate PR-B activity. Both 3-deoxycompounds, being selective ligands of progesterone membrane receptors, do not affect PR-B activity.
المشرفين على المادة: 0 (Receptors, Progesterone)
0 (progesterone receptor B)
4G7DS2Q64Y (Progesterone)
تواريخ الأحداث: Date Created: 20180509 Date Completed: 20180613 Latest Revision: 20180613
رمز التحديث: 20221213
DOI: 10.1134/S0006297918050103
PMID: 29738691
قاعدة البيانات: MEDLINE
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