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Also important in binding of E
2020-01-21
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 Introduction The cervix is a
2020-01-21
Introduction The GS967 is a poorly studied component of the mare’s reproductive tract. It has anatomical and biological defense mechanisms involved in the delicate balance between immunological tolerance, sperm transport and biological defense. Anatomically, the cervix is composed of epithelial
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Overall we found that all
2020-01-21
Overall, we found that all hormone treatment groups were able to learn spatial working and reference memory tasks, as shown by their performance across days on the WRAM (days 2–12, collapsed across the 4 trials) and the MWM (days 1–5, collapsed across the 4 trials). During the acquisition phase of t
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Angiomatoid fibrous histiocytoma originally described
2020-01-21
Angiomatoid fibrous histiocytoma (originally described as angiomatoid malignant fibrous histiocytoma) is a soft tissue tumor of intermediate biologic potential. AFH typically arises within extremity deep dermis and subcutis in children and young adults,157, 158, 159 but can arise in older adults and
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Elevated production of cysLTs in
2020-01-20
Elevated production of cysLTs in 5-Methyl-UTP and rhinitis in general and aspirin-sensitive disease in particular10, 11, 26, 27 has been implicated in causing epithelial cell activation and excessive mucus secretion, which characterize these diseases.2, 28 It is of particular interest, therefore, t
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PRT062607 Hydrochloride Nuclear export mediated by CRM
2020-01-20
Nuclear export mediated by CRM1 is initiated by an interaction between RanGTP and the HEAT9 loop of CRM1, triggering a conformational change in the NES binding site that permits NES–cargo protein binding (Dong et al., 2009, Fung and Chook, 2014). Our docking simulation results predicted that DP2392-
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Several highly selective COX inhibitors coxibs
2020-01-20
Several highly selective COX-2 inhibitors (coxibs) have been reported and marketed [6], including celecoxib [7] and etoricoxib [8] (Fig. 1). Even though these drugs produce less ulceration than conventional NSAIDs, coxibs still produce significant gastric and cardiovascular side effects due to the d
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Mouse Cyp a is a
2020-01-20
Mouse Cyp3a11 is a homologous isoform of the human CYP3A4 gene, and both are highly expressed in the liver (Hart, Cui, Klaassen, & Zhong, 2009). CYP3A4 is the most abundant CYP450 in hepatic microsomes responsible for drug and xenobiotic metabolism (Zanger & Schwab, 2013), and it is the most active
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br Conflict of interest br Acknowledgements This work
2020-01-20
Conflict of interest Acknowledgements This work was funded by the National Science Centre, Poland, grant number N N303 571539. We are greatly indebted to Patrick Fox for help with the final manuscript. Introduction Alkylating agents which interact directly with DNA to form covalent bonds h
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br Acknowledgements This work was supported by
2020-01-20
Acknowledgements This work was supported by grants from Agence Nationale de la Recherche (ANR CAPHE) and from Ligue contre le Cancer. We acknowledge the continuous support of CNRS and the University of Strasbourg. We thank the technical assistance of the “Plateforme de Chimie Intégrative de Stras
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In addition we investigated if
2020-01-20
In addition, we investigated if the previously reported papain inhibitor can inhibit rhodesain, and found that it was not active at inhibiting rhodesain. The vinyl sulfone analogue of () was then synthesized and tested, and it was also inactive towards rhodesain. We then determined the time depend
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As previously stated the most unexpected
2020-01-20
As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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BMS 193885 synthesis This work aimed to investigate whether
2020-01-20
This work aimed to investigate whether the increase in liver lipid depots, observed in the fetuses from rats fed a saturated-fat-rich diet, persists later in life in the offspring (a) at 21days of age immediately after weaning and (b) at 140days of age, after healthy nourishing. Furthermore, we want
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BMS 470539 dihydrochloride Sensory gating describes a filter
2020-01-20
‘Sensory gating’ describes a filter mechanism protecting the central nervous system from sensory overload by inhibiting behaviorally irrelevant input (Boutros et al., 2004, 2008). This permits BMS 470539 dihydrochloride to a changing contextual environment (Fruhstorfer et al., 1970; Grunwald et al.
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A recent study reports the expression of glutathione
2020-01-20
A recent study reports the expression of glutathione-dependent enzymes (GGT, GST-isoforms, gamma-glutamylcysteine synthetase, glutathione disulfide reductase and GSH peroxidase) in human primary PT AZD2932 in four subsequent passages [33]. In this study, we present phase I and II activities at mult
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