The influence of 17-oxo- and 17-hydroxy-16,17-secoestratriene derivatives on estrogen receptor
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Jovanovic-Santa, SPetrović, Julijana
Sakac, M
Žakula, Zorica
Isenović, Esma R.
Ribarac-Stepić, Nevena B.
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Since many of newly synthesised D-secoestratriene derivatives showed antiestrogenic effect, with almost a total loss of estrogenic activity, we studied the effects of some of these compounds on estrogen receptors (ER), the translocation of the estrogen-ER complexes formed in presence of competing substances into the nucleus, as well as the binding of these complexes to DNA. The results of uterotrophic effects of analysed derivatives are in agreement with the influence of these compounds on activity and binding parameters of estrogen receptors. Namely, compounds that show relatively high antiestrogenic activity predominantly increase K-d and inhibit translocation to nuclei of radioactive complexes formed in their presence. On the other hand, compounds that do not significantly change binding parameters of estrogen receptors do not show antiestrogenic effect in in vivo experiments.
Keywords:
steroids / estrogens / antiestrogens / D-secoestratriene derivatives / estrogen receptor binding / steroid-receptor interaction / receptor activation / nuclear translocationSource:
Collection of Czechoslovak Chemical Communications, 2006, 71, 4, 532-542
DOI: 10.1135/cccc20060532
ISSN: 0010-0765
WoS: 000236938200002
Scopus: 2-s2.0-33744949566
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VinčaTY - JOUR AU - Jovanovic-Santa, S AU - Petrović, Julijana AU - Sakac, M AU - Žakula, Zorica AU - Isenović, Esma R. AU - Ribarac-Stepić, Nevena B. PY - 2006 UR - https://vinar.vin.bg.ac.rs/handle/123456789/3007 AB - Since many of newly synthesised D-secoestratriene derivatives showed antiestrogenic effect, with almost a total loss of estrogenic activity, we studied the effects of some of these compounds on estrogen receptors (ER), the translocation of the estrogen-ER complexes formed in presence of competing substances into the nucleus, as well as the binding of these complexes to DNA. The results of uterotrophic effects of analysed derivatives are in agreement with the influence of these compounds on activity and binding parameters of estrogen receptors. Namely, compounds that show relatively high antiestrogenic activity predominantly increase K-d and inhibit translocation to nuclei of radioactive complexes formed in their presence. On the other hand, compounds that do not significantly change binding parameters of estrogen receptors do not show antiestrogenic effect in in vivo experiments. T2 - Collection of Czechoslovak Chemical Communications T1 - The influence of 17-oxo- and 17-hydroxy-16,17-secoestratriene derivatives on estrogen receptor VL - 71 IS - 4 SP - 532 EP - 542 DO - 10.1135/cccc20060532 ER -
@article{ author = "Jovanovic-Santa, S and Petrović, Julijana and Sakac, M and Žakula, Zorica and Isenović, Esma R. and Ribarac-Stepić, Nevena B.", year = "2006", abstract = "Since many of newly synthesised D-secoestratriene derivatives showed antiestrogenic effect, with almost a total loss of estrogenic activity, we studied the effects of some of these compounds on estrogen receptors (ER), the translocation of the estrogen-ER complexes formed in presence of competing substances into the nucleus, as well as the binding of these complexes to DNA. The results of uterotrophic effects of analysed derivatives are in agreement with the influence of these compounds on activity and binding parameters of estrogen receptors. Namely, compounds that show relatively high antiestrogenic activity predominantly increase K-d and inhibit translocation to nuclei of radioactive complexes formed in their presence. On the other hand, compounds that do not significantly change binding parameters of estrogen receptors do not show antiestrogenic effect in in vivo experiments.", journal = "Collection of Czechoslovak Chemical Communications", title = "The influence of 17-oxo- and 17-hydroxy-16,17-secoestratriene derivatives on estrogen receptor", volume = "71", number = "4", pages = "532-542", doi = "10.1135/cccc20060532" }
Jovanovic-Santa, S., Petrović, J., Sakac, M., Žakula, Z., Isenović, E. R.,& Ribarac-Stepić, N. B.. (2006). The influence of 17-oxo- and 17-hydroxy-16,17-secoestratriene derivatives on estrogen receptor. in Collection of Czechoslovak Chemical Communications, 71(4), 532-542. https://doi.org/10.1135/cccc20060532
Jovanovic-Santa S, Petrović J, Sakac M, Žakula Z, Isenović ER, Ribarac-Stepić NB. The influence of 17-oxo- and 17-hydroxy-16,17-secoestratriene derivatives on estrogen receptor. in Collection of Czechoslovak Chemical Communications. 2006;71(4):532-542. doi:10.1135/cccc20060532 .
Jovanovic-Santa, S, Petrović, Julijana, Sakac, M, Žakula, Zorica, Isenović, Esma R., Ribarac-Stepić, Nevena B., "The influence of 17-oxo- and 17-hydroxy-16,17-secoestratriene derivatives on estrogen receptor" in Collection of Czechoslovak Chemical Communications, 71, no. 4 (2006):532-542, https://doi.org/10.1135/cccc20060532 . .