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Another potential source of variable affinities is inherent
2021-02-27
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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br The modulation of ER from SERMs to
2021-02-27
The modulation of ERα: from SERMs to TSECs Continued efforts to provide women with efficacious menopausal therapies have generated interest in the development of selective Kif15-IN-2 receptor modulators (SERMs). Similar to estrogens, SERMs have been shown to bind to ERs with high affinity, despi
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Introduction Primitive neuroectodermal tumors PNETs are
2021-02-27
Introduction Primitive neuroectodermal tumors (PNETs) are malignant, small round cell tumors of neural crest origin which typically arises from bone or soft tissue in the trunk/axial skeleton/paraspinal regions in adolescents and young adults and comprises of 50% cases with local recurrence and met
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Treatment with AAV EP also improved aspects of
2021-02-27
Treatment with AAV9-EP4 also improved aspects of adverse cardiac remodeling. The increased collagen deposition noted in the peri infarct and remote zone after MI was substantially attenuated by use of AAV9-EP4 and there were significant reductions in the number of macrophages and T MLN 9708 infiltr
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Compounds and possessed relatively low clogP values and
2021-02-27
Compounds 11–13 and 15 possessed relatively low clogP values and tended to show relatively weak antagonist activity regardless of their potent EP1 receptor affinity. Compounds 2–4, which were selected based on their potent in vivo antagonist activity, were found to be effective in an animal model.
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br Materials and methods br Results br Discussion
2021-02-27
Materials and methods Results Discussion Ubiquitination is an important eukaryotic process that defines the fate of proteins and their functionality. It has multiple roles in cell survival, differentiation and development (Glickman and Ciechanover, 2002). Ubiquitination is usually known as
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ICT is a product of
2021-02-27
ICT is a product of icariin via the metabolism of intestinal bacteria with estrogen-like activities [33]. ICT as a bone-protecting agent can enhance osteoblast differentiation while suppressing osteoclastic differentiation in vitro [19], and stimulate osteogenic differentiation and inhibit adipogene
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In addition to glutamatergic inputs the RTn integrates
2021-02-26
In addition to glutamatergic inputs, the RTn integrates cholinergic, serotonergic and noradrenergic synapses of fibers coming from nuclei located in the brainstem (Asanuma, 1992, Morrison and Foote, 1986, Pare et al., 1988) involved in the alternating firing mode and in the frequency changes of reti
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br Discussion Cytomegalovirus CMV is
2021-02-26
Discussion Cytomegalovirus (CMV) is a herpes virus that causes primary infection in normal hosts and re-activation infection in compromised hosts with impaired CMI, e.g., organ transplants. Following primary infection, which may be severe, CMV becomes latent in lymphocytes. Reactivation may occur
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To determine the time course of ZD
2021-02-26
To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour VAS2870 were exposed to the drug for 10, 30 or 60 min. The levels of DNA interstrand cross-links in HT29 or LS174T cells did not increase with exposure time, suggesting that ZD27
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Rambabu et al reported A series
2021-02-26
Rambabu et al. reported A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives synthesized from readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and further reacted with different substituted am
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There are some limitations to our study First the small
2021-02-26
There are some limitations to our study. First, the small sample size, even if comparable or higher than most studies, did not offer the possibility to consider other variables, such as frequency of use or age of onset. Second, since most subjects did not report current use, we could not analyze sep
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Enlarging the ligand binding pocket by reduction of the
2021-02-26
Enlarging the ligand-binding pocket by reduction of the size of the residue F435 switched DES to an agonist indicating that F435 is involved in mediating the antagonistic effect of DES (Fig. 7E) [13]. The conformation of the smaller side chain of L435 was either not altered by DES or was too small t
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Similarly EGCG restored the mitochondrial energy shortfall
2021-02-26
Similarly, EGCG restored the mitochondrial energy shortfall in fibroblasts and lymphoblasts of the patients affected by Down syndrome, even so the mechanism of the effect was not clearly known (Valenti et al., 2013). EGCG also stimulated the mitochondrial biogenesis by activation of nuclear respirat
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EP EP and EP receptor expression on HMVEC L was
2021-02-26
EP1, EP3 and EP4 receptor expression on HMVEC-L was shown recently by flow cytometry [14]. However, only EP4 mRNA expression was previously described in these cells [49]. Our data obtained with RT-PCR showed EP4 mRNA and very low levels of EP1 mRNA, but no EP2 and EP3 mRNA expression was detectable
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