FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2065521005> ?p ?o ?g. }

• W2065521005 endingPage "122" @default.
• W2065521005 startingPage "111" @default.
• W2065521005 abstract "The specific pharmacological profile of the 19-norprogestin nomegestrol acetate (NOMAC) is, at least in part, defined by its pattern of binding affinities to the different steroid hormone receptors. In the present study, its affinity to the progesterone receptor (PgR), the androgen receptor (AR) and the estrogen receptor (ER) was re-evaluated and compared to those obtained for progesterone (P) and several progestins. The characteristics of binding to the PgR in rat uterus were determined and Ki were found to be roughly similar with 22.8 and 34.3 nM for NOMAC and P, respectively. The binding characteristics of 3H-NOMAC were also determined and compared to that of 3H-ORG2058 with Kd of 5 and 0.6 nM, respectively for rat uterus and 4 and 3 nM, respectively for human T47-D cells. Structure–affinity and –activity relationships were studied on a variety of compounds related to NOMAC in order to assess its specificity as a progestin. The effects of NOMAC on the binding of androgen to the AR were investigated, using rat ventral prostate as target model. Contrary to what was observed for MPA, the RBA of NOMAC was found to decline with time, showing anti-androgenic rather than androgenic potential, a result that was confirmed in vivo. Regarding the ER, since none of the progestins were able to compete with estrogen for binding in rat uterus as well as in Ishikawa cells, the induction of alkaline phosphatase activity (APase) was used as an estrogen-specific response. It confirmed the intrinsic estrogenicity of progestins derived from 19-nor-testosterone (19NT), norethisterone acetate (NETA), levonorgestrel (LNG) or norgestimate (NGM) and others. In contrast, all P and 19-norP derivatives remained inactive. Finally, to complete this overview of NOMAC at the sex steroid receptor levels, the lack of estrogenic or estrogenic-like activity was checked out in different in vitro models. Data from this study have demonstrated that NOMAC is a progestin that has greater steroid receptor selectivity compared to MPA or some other synthetic progestins. It may provide a better pharmacological profile than those progestins currently in use in HRT and OC." @default.
• W2065521005 created "2016-06-24" @default.
• W2065521005 creator A5003385146 @default.
• W2065521005 creator A5014461731 @default.
• W2065521005 creator A5019706619 @default.
• W2065521005 creator A5039500826 @default.
• W2065521005 creator A5075168635 @default.
• W2065521005 creator A5079584430 @default.
• W2065521005 creator A5091547651 @default.
• W2065521005 date "2003-11-01" @default.
• W2065521005 modified "2023-09-27" @default.
• W2065521005 title "An overview of nomegestrol acetate selective receptor binding and lack of estrogenic action on hormone-dependent cancer cells" @default.
• W2065521005 cites W1523966773 @default.
• W2065521005 cites W1537475508 @default.
• W2065521005 cites W1593442063 @default.
• W2065521005 cites W162092248 @default.
• W2065521005 cites W1810492880 @default.
• W2065521005 cites W1966587329 @default.
• W2065521005 cites W1967164065 @default.
• W2065521005 cites W1968150567 @default.
• W2065521005 cites W1970287724 @default.
• W2065521005 cites W1970703128 @default.
• W2065521005 cites W1973976424 @default.
• W2065521005 cites W1980766186 @default.
• W2065521005 cites W1987160428 @default.
• W2065521005 cites W1990594056 @default.
• W2065521005 cites W2005354991 @default.
• W2065521005 cites W2010155859 @default.
• W2065521005 cites W2011963162 @default.
• W2065521005 cites W2012041763 @default.
• W2065521005 cites W2016680209 @default.
• W2065521005 cites W2028287922 @default.
• W2065521005 cites W2028706115 @default.
• W2065521005 cites W2032248685 @default.
• W2065521005 cites W2035787815 @default.
• W2065521005 cites W2036891631 @default.
• W2065521005 cites W2038302740 @default.
• W2065521005 cites W2044212803 @default.
• W2065521005 cites W2050219190 @default.
• W2065521005 cites W2053471894 @default.
• W2065521005 cites W2055430160 @default.
• W2065521005 cites W2060281353 @default.
• W2065521005 cites W2073874962 @default.
• W2065521005 cites W2081663679 @default.
• W2065521005 cites W2082111982 @default.
• W2065521005 cites W2082559087 @default.
• W2065521005 cites W2088439448 @default.
• W2065521005 cites W2090094748 @default.
• W2065521005 cites W2094208265 @default.
• W2065521005 cites W2100372858 @default.
• W2065521005 cites W2111513204 @default.
• W2065521005 cites W2118760305 @default.
• W2065521005 cites W2122104479 @default.
• W2065521005 cites W2124653687 @default.
• W2065521005 cites W2130180306 @default.
• W2065521005 cites W2148576257 @default.
• W2065521005 cites W2152374768 @default.
• W2065521005 cites W2157182591 @default.
• W2065521005 cites W2170108604 @default.
• W2065521005 cites W2171148899 @default.
• W2065521005 cites W3022279537 @default.
• W2065521005 cites W36626011 @default.
• W2065521005 cites W4231298489 @default.
• W2065521005 cites W4241185965 @default.
• W2065521005 cites W4245176921 @default.
• W2065521005 cites W4245804455 @default.
• W2065521005 cites W4252221156 @default.
• W2065521005 cites W4253904058 @default.
• W2065521005 cites W86329342 @default.
• W2065521005 doi "https://doi.org/10.1016/j.jsbmb.2003.08.003" @default.
• W2065521005 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/14672731" @default.
• W2065521005 hasPublicationYear "2003" @default.
• W2065521005 type Work @default.
• W2065521005 sameAs 2065521005 @default.
• W2065521005 citedByCount "21" @default.
• W2065521005 countsByYear W20655210052012 @default.
• W2065521005 countsByYear W20655210052013 @default.
• W2065521005 countsByYear W20655210052014 @default.
• W2065521005 countsByYear W20655210052015 @default.
• W2065521005 countsByYear W20655210052017 @default.
• W2065521005 countsByYear W20655210052018 @default.
• W2065521005 countsByYear W20655210052019 @default.
• W2065521005 countsByYear W20655210052022 @default.
• W2065521005 crossrefType "journal-article" @default.
• W2065521005 hasAuthorship W2065521005A5003385146 @default.
• W2065521005 hasAuthorship W2065521005A5014461731 @default.
• W2065521005 hasAuthorship W2065521005A5019706619 @default.
• W2065521005 hasAuthorship W2065521005A5039500826 @default.
• W2065521005 hasAuthorship W2065521005A5075168635 @default.
• W2065521005 hasAuthorship W2065521005A5079584430 @default.
• W2065521005 hasAuthorship W2065521005A5091547651 @default.
• W2065521005 hasConcept C121608353 @default.
• W2065521005 hasConcept C126322002 @default.
• W2065521005 hasConcept C134018914 @default.
• W2065521005 hasConcept C170493617 @default.
• W2065521005 hasConcept C185592680 @default.
• W2065521005 hasConcept C2776607906 @default.
• W2065521005 hasConcept C2776888042 @default.

• next