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Also important in binding of
2020-01-20
Also important in binding of E2 to the ER is the hydroxyl on the D ring, which has a stabilizing contact with His-524 in ERα (Fig. 7) and with His-475 in ERβ (Fig. S1) [8,9,36,37]. The spatial relationship of the functional groups on the A and D rings on E2 has been used to develop chemicals contai
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br The estrogen receptors History and discovery In Elwood
2020-01-20
The estrogen receptors: History and discovery In 1958, Elwood Jensen discovered the estrogen receptor, the first receptor ever encountered for any hormone, by showing that reproductive female tissues were able to uptake estrogen from the circulation by binding to proteins. He later demonstrated t
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br Discussion The etiology of autoimmune diseases including
2020-01-20
Discussion The etiology of autoimmune diseases including psoriasis is intricate and a composite of environmental and biological factors. There are very limited studies available that report the association analysis of ACE I/D polymorphism with psoriasis risk. In the current study we report on ass
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When six chemical inhibitors were incubated with
2020-01-20
When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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The pharmacokinetics properties of compound were evaluated i
2020-01-20
The pharmacokinetics properties of compound were evaluated in male Sprague Dawley rats following IV (0.7mg/kg) and oral (2.0mg/kg) dosing. The total body clearance and the terminal half-life were 0.73 L/h/kg and 5.1h, respectively. After oral administration the compound showed good bioavailability
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This study evaluated the role of SERT in classica
2020-01-20
This study evaluated the role of SERT in classical fear conditioning using a SERT knockout rat model. We found a clear disruption of cue-conditioned fear in SERT−/− rats, as measured with the fear-potentiated startle. This disruption was due to a deficit in fear acquisition and was accompanied by de
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Previous studies showed that many steroidogenic enzymes act
2020-01-19
Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although
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br Conclusion br Acknowledgements br Introduction In recent
2020-01-19
Conclusion Acknowledgements Introduction In recent years, fast progress has been made toward using the supercritical technology in industrial separation processes. Apart from a green extraction process that replaces organic solvents, applications involving supercritical fluids include super
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ClC is a member of the
2020-01-19
ClC-3 is a member of the voltage-gated chloride channel superfamily and has many roles in cell proliferation, apoptosis, Caspase-3, human recombinant proteinase progression and so on (Dai et al., 2005). A growing number of studies showed that ClC-3 encoded a volume-regulated Cl− channel (ICl,Vol) i
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The new ESC guidelines incorporate
2020-01-19
The new ESC guidelines incorporate data from a network meta-analysis of 100 studies confirming that new-generation drug-eluting stents (DES) improve survival compared with medical treatment, although this has not been demonstrated in any individual study. REVASCULARIZATION IN NON–ST-ELEVATION ACU
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Our study shows that deletion of Dpf in
2020-01-19
Our study shows that Fructose Colorimetric/Fluorometric Assay Kit of Dpf2 in mouse ESCs decreased their self-renewal ability and dramatically impaired their differentiation into mesoderm and endoderm while promoting neural ectoderm differentiation. The differentiation defect to meso-endoderm could b
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Given the potency enhancing effect of the
2020-01-19
Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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Another potential source of variable affinities is inherent
2020-01-17
Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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Our observation that nuclear but not cytoplasmic EP expressi
2020-01-17
Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant Norethindrone synthesis whereas cytoplasmic EP4 was commonly observed [13]. While G prot
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br Materials and methods br Results br Discussion
2020-01-17
Materials and methods Results Discussion Our results based on the Y2H analysis between the U-box-motif region of E3s and the UBC domain of E2s showed that, among 40 rice E2s, 11 E2s accounted for 70% of the interactions with 17 ARM-U-box E3 Ub-ligases (Fig. 2, Fig. 3). These 11 E2s belong t
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