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In rodent models the loss of estrogens through ovariectomy h
2019-10-16
In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an Volasertib receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitric oxide synthase in
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PR171 Despite the sources of error
2019-10-15
Despite the sources of error discussed above, several trends have emerged and much valuable data are available regarding binding affinities of progestogens for different steroid receptors. All the progestogens bind to the PR with a high affinity, typically in the nanomolar range. For example the syn
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Moreover considering that several polyphenols and flavonoids
2019-10-15
Moreover, considering that GSK 5959 several polyphenols and flavonoids (i.e. chalcones, flavanones, resveratrol derivatives, ellagic acid) are reported to inhibit tyrosinase and elastase (Pillaiyar et al., 2017; Xing et al., 2016; Wittenauer et al., 2015), the relations between enzyme inhibitory act
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Recently cross talk between DDR and the
2019-10-15
Recently, cross-talk between DDR2 and the insulin receptor and between Notch1 and DDR1 was proposed. Stimulation of cells with collagen I and insulin promotes Tyr740 as well as total tyrosine phosphorylation of DDR2 receptor to a greater extent than the phosphorylation stimulated by collagen I alone
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br Introduction Natural killer NK cells have an
2019-10-15
Introduction Natural killer (NK) cells have an unique ability to directly lyse transformed, virus-infected or stressed cells without prior sensitization or major histocompatibility complex (MHC) class I restriction [1], [2]. They were initially defined and shown to be important effectors of the i
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Self Determination Theory SDT as described by Ryan
2019-10-15
Self-Determination Theory (SDT), as described by Ryan and Deci (2000) is “an approach to human motivation and personality that uses traditional empirical methods while employing an organismic metatheory highlighting the importance of humans\' evolved inner resources for personality development and b
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Several studies suggest that the beneficial metabolic effect
2019-10-15
Several studies suggest that the beneficial metabolic effects of adiponectin in humans are primarily mediated by its HMW isoform. Increases in the ratio of HMW to total adiponectin, but not the total adiponectin level, correlated well with improved apexbio dilution sensitivity during treatment with
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Immune modulation by steroid hormones is a rather new
2019-10-15
Immune modulation by steroid hormones is a rather new aspect of the research on endocrine interactions in lower vertebrates (Harris and Bird, 2000). In the classical view, steroids exert their effects by binding to specific intracellular receptors that function as ligand-activated transcriptional re
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Targeting the MAPK pathway has attracted significant interes
2019-10-15
Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have
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The compounds listed in Table Table Table Table Table
2019-10-15
The compounds listed in Table 1, Table 2, Table 3, Table 4, Table 5 were biologically evaluated for their inhibition of the specific binding of a radiolabeled ligand [3H]PGE2 to membrane fractions prepared from cells stably expressing each mouse prostanoid receptor. The EP1 antagonist activity of th
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The monomeric oligomeric states of
2019-10-15
The monomeric/oligomeric states of DDR2-V5-His and DDR2-Fc were confirmed by Western blotting under reducing and non-reducing conditions. As shown in Fig. 1b, DDR2-V5-His exhibited a relative molecular mass of ~60 kDa under both reducing and non-reducing conditions, consistent with this protein bein
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In vitro studies in NSCLC cell lines expressing EGFR mutants
2019-10-15
In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC angiotensin ii with Growth inhibition (GI50) values ranging from 7 to 32 nmo
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Patients and methods This study was performed at academic ce
2019-10-14
Patients and methods This study was performed at 3 academic centers (Chung-Ang University YongSan Hospital, Soonchunhyang University Hospital, and Chung-Ang University Hospital) in Seoul, Korea, from November 2008 to November 2010. The study protocol was approved by the institutional review boards
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In our former work our
2019-10-14
In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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br Substrate Specificity Discrimination and Binding Energy I
2019-10-14
Substrate Specificity, Discrimination, and Binding Energy In R 568 hydrochloride to catalytic efficiency, which can be gauged in reference to an absolute scale of ‘catalytic perfection’ 10, 11, specificity is a relative concept because it requires comparison between given alternative substrates.
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