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Prenylation may turn a flavonoid from an agonist
2020-04-07
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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The mechanisms by which coregulators control the actions of
2020-04-07
The mechanisms by which coregulators control the actions of estrogen receptors are still a topic of ongoing research. From studies in cancer cells, we have learned that a large group of coregulators have specific structural motifs that than affect their contact with ER ligand-binding domains (Heery,
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br Introduction Receptor tyrosine kinases RTKs are criticall
2020-04-07
Introduction Receptor tyrosine kinases (RTKs) are critically involved in the development and progression of human cancers and are therefore useful targets for anti-cancer therapies [1]. The Eph receptors represent the largest subfamily of receptor protein kinases and interact with ligands called
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Multiple technologies exist for analyzing the contents of si
2020-04-07
Multiple technologies exist for analyzing the contents of single cells, including single-cell DNA sequencing, RNA expression analysis, and protein level and activity measurements (Hu et al., 2018; Narrandes & Xu, 2018; Ortega et al., 2017; Wang & Navin, 2015). Single-cell DNA sequencing is generally
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A spectrum of therapies came
2020-04-07
A spectrum of therapies came in order to counter this misfortune, some of them are discussed below. However, the common problem faced by most of these drugs is their emerging resistance after a span of time. Some of the important drugs reported so far are as: Quinine-based antimalarial drugs (Fig. 1
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The in vivo IC M in the
2020-04-07
The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free dinacic
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Regarding the effects of CRF on anxiety
2020-04-07
Regarding the effects of CRF on anxiety, Sahuque et al. (2006) have demonstrated that this neuropeptide also enhances anxiety when injected into the bed nucleus of the stria terminalis (BNST), a (±)-CPSI 1306 australia structure that has also been related to defensive behavior (Casada and Dafny, 19
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Moxifloxacin This study has several limitations
2020-04-07
This study has several limitations. First, despite the relatively large number of participants for a pharmacological neuroimaging study, sample sizes for examining the modulation of THC effects by COMT Moxifloxacin were small. Therefore, these particular findings should be interpreted with caution a
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Rat pheochromocytoma PC cells have been
2020-04-06
Rat pheochromocytoma PC12 cells have been widely used as a cell system to study intracellular signaling leading to neurite outgrowth. The advantages of using PC12 cells in the CHK studies are the fact that they naturally express the rat form of CHK and the observation that down-regulation of CHK fun
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ABT 724 trihydrochloride Neonatal hydronephrosis induced by
2020-04-06
Neonatal hydronephrosis induced by TCDD exposure via lactation has a critical window for onset: the incidence of this disease peaks around PNDs 1–4, followed by a rapid decrease to a substantially null level in adulthood (Couture-Haws et al., 1991; Yoshioka et al., 2016). The EP1 protein was localiz
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Introduction Obesity constitutes a global healthcare problem
2020-04-06
Introduction Obesity constitutes a global healthcare problem and has many adverse effects on the cardiovascular function [1,2]. Recently, the perivascular adipose tissue (PVAT) has emerged as a relevant fat depot for cardiovascular risk and as a potential trigger in vascular dysfunction. Indeed, PV
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br Results br Discussion Mucosal barriers are constitutively
2020-04-06
Results Discussion Mucosal barriers are constitutively challenged by various stimuli, and the homeostasis of mucosal barriers both at steady state and upon challenge are maintained by tissue-resident immune Brefeldin A (Kurashima et al., 2013, Okumura and Takeda, 2016). ILC3s are found in lym
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br Experimental Procedures br Author
2020-04-06
Experimental Procedures Author Contributions Acknowledgments Introduction Oxysterols came to prominence in the late 1970\'s with the oxysterol hypothesis which proposed that the suppressive effect of cholesterol on its own synthesis is mediated through oxysterols not by cholesterol itsel
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br Materials and methods br
2020-04-06
Materials and methods Results and discussion Concluding remarks Together, the results of the theoretical kinetic simulations and of the analysis of the experimentally determined kinetic data of SoBADH performed in this work show that ignoring substrate inhibition causes potentially importan
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Next the BE obtained for the different complexes
2020-04-06
Next, the BE obtained for the different complexes were evaluated. From the BE obtained from our MD simulations, a very good binder can be differentiated from a very weak binder (−11.85 kcal/mol for MTX vs. −6.74 and −3.61 kcal/mol for compounds 14b and 15c, respectively) but ligands with similar bin
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