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p-Carborane bisphenols and their derivatives were prepared and evaluated for binding affinity to estrogen receptor α.
HER2 might be associated with growth dependence of the tumor cells, but ERβ2 seems to be associated with binding affinity to estrogen and DNA.
Future investigations should clarify the role of bladderwrack and other seaweed species on estrogen and progesterone metabolism, to evaluate its potential binding affinity to estrogen and progesterone receptors, and to determine its effects on proliferation in hormone-sensitive tissues.
In humans only 30 50% of the population harbour the bacteria capable of converting daidzein to equol, and this metabolite has biological activities that differ from its parent compound, e.g. relative binding affinity to estrogen receptors (Cassidy et al., 1994; Duncan et al., 1999; Lampe, 2009).
Musks show low binding affinity to estrogen receptors, and their environmental impact as endocrine disruptors through this pathway is also regarded as low (Bitsch et al. 2002; Chou and Dietrich 1999a), although indirect endocrine effects such as inhibition of hormone synthesis (Kester et al. 2000; Sanderson et al. 2001) have not been examined.
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Derivatives with a hydroxy group at the molecular edge exhibit potent binding affinity to the estrogen receptor α (ERα) and ERβ (IC50 < μM), while binding to the estrogen-related receptor γ (ERRγ), i.e., an orphan nuclear receptor on which estrogens often trigger unfavorable events, was not observed.
Its high binding affinity to the estrogen receptor (S-equol preferentially activates ERβ) [ 108, 109, 112] has been used to alleviate the symptoms of menopause [ 107].
We assessed the relative binding affinity to the estrogen receptor of the selected phytoestrogens coumestrol, genistein, daidzein, and the putative phytoestrogen mangostin compared to estradiol by a competitive Scatchard analysis.
The relative binding affinities to the estrogen receptors (ERα and ERβ) was assessed by a competitive radiometric assay.
BPA is considered a weak estrogen because its binding affinity to ER α and ER β was estimated to be >1000 10 000-fold lower than the natural hormone E2.
In the past, BPA was considered a "weak" estrogen because of its low binding affinity to both ERα and ERβ [18], [19], as well as for having a low transcriptional activity through these ERE binding receptors [40].
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