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Binding affinity was measured by a scintillation proximity b
2019-09-11

Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six
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To understand more clearly how
2019-09-11

To understand more clearly how these activities are combined in the heterotrimeric enzyme and to understand more clearly how DNA alkylation might effect DNA helicase activity, we summarize the relevant features of the structure of RecBCD determined in the presence of DNA. The RecB and RecC subunits
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br Allosteric inhibitors In general candidate
2019-09-11

Allosteric inhibitors In general, candidate drugs that bind to a GPCR at a site that is distinct (allosteric site) from the binding site of the endogenous agonist (orthosteric site) are attracting increasing attention 39, 42, 58. Allosteric modulators display saturability of their effect, probe d
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br Conclusions This report describes the
2019-09-10

Conclusions This report describes the discovery of a new class of host-directed antiviral agents characterized by a 1-aryl-4,6-diamino-1,2-dihydrotriazine scaffold, responsible for a host (human) DHFR inhibition mechanism. Host-targeting antivirals represent an alternative and emerging strategy t
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There is literature precedence for the metabolic activation
2019-09-10

There is literature precedence for the metabolic activation of the methylene carbons adjacent to the ring oxygen(s) of dioxanes and benzopyrans resulting in ring-opened electrophilic carbonyl species. Based on the potential for this metabolic pathway being operative with , a steric block approach wa
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Previous studies found that depression primarily results fro
2019-09-10

Previous studies found that depression primarily results from impaired monoaminergic neurotransmission systems [1], [2]. The glutamatergic and GABAergic systems as well as several neuropeptide systems have also been the focus of pathophysiological studies on depression [1], [2]. Inflammatory cytokin
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There are some limitations to our
2019-09-10

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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br Acknowledgements This work was supported
2019-09-10

Acknowledgements This work was supported by a grant from the Deutsche Forschungsgemeinschaft to Uwe Knippschild and Martin Wabitsch (SFB 1149/B4). P. Fischer-Posovszky is funded by a Margarete von Wrangell scholarship financed by the Ministerium für Wissenschaft, Forschung und Kunst Baden-Württem
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Two isoforms of intracellular ER ER and ER after binding
2019-09-10

Two isoforms of intracellular ER, ERα, and ERβ, after binding to estrogens and translocate to the nucleus, activate some transcription factors and signaling pathways. The deregulation of estrogenic pathways can elevate transcriptional activity contributed to the development of cancer. Expression of
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Introduction Fish commonly employ pheromones to regulate a v
2019-09-10

Introduction Fish commonly employ pheromones to regulate a variety of functions including reproductive communication [1]. Reproductive pheromones induce both primer effects, such as changes in the endocrine or physiological state of conspecifics, and releaser effects such as rapid behavioral respon
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In addition to vasoconstrictor actions acute effects ET exer
2019-09-10

In addition to vasoconstrictor actions (acute effects), ET-1 exerts potent mitogenic actions on vascular smooth muscle cells and cardiac myocytes (chronic effects), hence causing vascular and cardiac hypertrophy [19,24,25]. These effects are mediated via stimulation of either ETA or ETB receptors, a
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It is interesting to note that our results show
2019-09-10

It is interesting to note that Fmoc-Thr(tBu)-OH our results show a very similar behavior in binding of DDR2 ECD to immobilized a-telo (bovine-dermal) versus telo- (rat-tail) collagen I as a function of its oligomeric state. Thus, the telopeptide region of tropocollagen exerts little influence on DD
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br Methods An ongoing prospective
2019-09-10

Methods An ongoing prospective study at the Princess Margaret Cancer Centre is enrolling consenting patients with stage IV EGFRm NSCLC for longitudinal blood collection. Patients may enrol at any point in their treatment. In this study, we performed a cross-sectional analysis of 72 patient liquid
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The host virus coexistence is completely dependent on
2019-09-10

The host-virus coexistence is completely dependent on the balance between a strong immune response inhibiting virus replication and immune evasion and survival of the virus with periodic shedding to enable transmission to new hosts. In the process of ensuring this balance, the virus manipulates 7TM
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br Results and Discussion br Conclusions Understanding the
2019-09-10

Results and Discussion Conclusions Understanding the connections between function and fitness is a primary goal of many biological disciplines including systems biology and molecular evolution. While sound approaches have been developed to understand the connections between function and fitnes
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