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Soon after the discovery of ET and the cloning
2021-08-30
Soon after the discovery of ET1 and the cloning of its ETA and ETB receptors, low-molecular-weight compounds were identified that can prevent the binding and effects of radioactively labeled ET1 3, 5, 6, 8. Initially, these ERAs resulted from screening efforts (e.g. BQ123 39, 49 and bosentan [50]).
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In rodent models the loss of estrogens through ovariectomy h
2021-08-30
In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an X-Gal receptor receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitric oxide synthas
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To identify and characterize new possible molecular targets
2021-08-30
To identify and characterize new possible molecular targets, the mechanisms of various kinds of TCDD toxicities that occur by abnormal regulation in the downstream of AhR signals have been studied (Yoshioka et al., 2011). Experimental evidence has revealed that prostanoids (i.e., prostaglandins and
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To provide a brief critical
2021-08-30
To provide a brief critical evaluation of this technology and an outlook, we note that performance of SMEPT is critically dependent on each of the components making up this platform, namely the substrate, the enzyme, and the prodrug. With regards to the latter, SMEPT is built on the experience and s
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Several studies have demonstrated that Syn specifically asso
2021-08-30
Several studies have demonstrated that αSyn specifically associates with lipid rafts (Cole et al., 2002), raising the possibility that the perturbation of rafts can affect the aggregation and phosphorylation of αSyn (Fortin et al., 2004). Schneider et al. (2010) described the potential involvement o
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A major finding to emerge from
2021-08-30
A major finding to emerge from this study is a conserved regulatory scheme deployed by both innate and adaptive lymphocytes, which is coordinated by a cohort of TFs. The scheme functionally compartmentalizes effector IMD 0354 sale that circulate between blood and peripheral tissues from self-renewi
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While the mechanism of DHODH inhibition induced
2021-08-30
While the mechanism of DHODH inhibition-induced differentiation is not fully understood, this phenomenon may be caused by pyrimidine depletion. Pyrazofurin, an inhibitor of OMP decarboxylase, was able to induce differentiation and suggests pyrimidine depletion as a potential mechanism (Sykes et al.,
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We had earlier reported that collagen fibers with
2021-08-28
We had earlier reported that collagen fibers with intact native banded structure were occasionally observed in the kinase-deficient, membrane-anchored DDR2 ECD (DDR2/-KD) samples; however, in our DDR1/ECD and DDR2/ECD samples, observation of native banded structure of collagen was far more infrequen
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Altogether we have shown the presence
2021-08-28
Altogether we have shown the presence of fully methylated DAPK fragments in serum of ovarian cancer patients but also of women with uterine leiomyoma. This indicates the prerequisite for the analysis of not only healthy controls but also of women with other frequent non-cancer disease for the valida
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During the course of our research on mGlu
2021-08-28
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology
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br Materials and Methods br Results
2021-08-28
Materials and Methods Results Discussion Even though T cell checkpoint inhibitors alone have achieved impressive clinical benefit in some cancers, their application as single agents has had limited efficacy (Hamid et al., 2013; Wolchok et al., 2013). The resistance to immunotherapy is in pa
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Our approach relied on measurement of bulk solute
2021-08-28
Our approach relied on measurement of bulk solute diffusivity in the three tissue types of interest. Our diffusivity values (Table 3) are on the order of 10−6 cm2/s and are comparable to the PG diffusion coefficient in water at infinite dilution, which is about 10−5 cm2/s at room temperature, as wel
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The present study sought to determine if
2021-08-28
The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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br Conclusions br Introduction Today just as for the
2021-08-28
Conclusions Introduction Today – just as for the past 50 years – the most commonly used repellent in the world is DEET (Fradin, 1998; Pickett et al., 2008). The active ingredient, N,N-Diethyl-m-toluamide, is an oily synthetic substance applied topically to the skin in order to alter the host f
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For these reasons molecules of the ET family and in
2021-08-28
For these reasons, molecules of the ET family and in particular ET-1 are considered useful factors in the evaluation of malignancy and in consequence, in the prognosis for several forms of neoplasia, such as ovarian (Bagnato et al., 2005), prostate (Nelson et al, 1995, Nelson et al, 1996), colorecta
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