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br Introduction Breast cancer is the most common
2019-10-21
Introduction Breast cancer is the most common cancer in women and one of the leading causes of death worldwide. Estrogen receptor alpha (ERα, “wild-type” estrogen receptor), encoded by the estrogen receptor1 (ESR1) gene, is expressed in approximately 70% of all breast cancers. Hormonal therapy ha
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To study systemic potential of
2019-10-21
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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The development of novel approaches to study
2019-10-21
The development of novel approaches to study GPCR-mediated transactivation in live INO-1001 receptor is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment
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Crystallographic and NMR based analyses have revealed that
2019-10-21
Crystallographic and NMR-based analyses have revealed that RINGs and U-boxes have a common mode of interaction with E2s (Fig. 2A). The key structural elements are two loop-like regions, which, in the case of RINGs, coordinate Zn. The loops surround a shallow groove formed by the central α-helix. Tog
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Although PD is traditionally viewed as a motor
2019-10-21
Although PD is traditionally viewed as a motor disorder, evidence from numerous epidemiologic (Shiba et al., 2000) as well as case–control studies (Richard, 2005) suggest the occurrence of non-motor symptoms including hyposmia/anosmia, gastrointestinal disturbances, sleep abnormalities, autonomic dy
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Many filarial species harbor an endosymbiotic bacterium of t
2019-10-19
Many filarial species harbor an endosymbiotic bacterium of the genus Wolbachia. A recent investigation of Wolbachia distribution in 35 filarial species including 28 species and 7 genera and/or subgenera have shown that 37% of them harbor Wolbachia (Ferri et al., 2011). In filarial nematodes, Wolbach
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In the present study the expression of the
2019-10-19
In the present study, the GYKI 52466 dihydrochloride kinase of the CYP2C11 gene and the levels of its protein and activity were decreased in rats with liver insufficiency and in rats after induced dysfunction of the serotonergic system during normal liver function. Moreover, serotonergic system dys
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To assess which export pathway is used by the
2019-10-19
To assess which export pathway is used by the iNOS mRNA, we inhibited CRM1 activity by incubation of DLD-1 fura kinase with LMB. Since LMB covalently and exclusively binds to CRM1, it represents a potent and specific inhibitor of the CRM1 transport activity [38]. Inhibition of CRM1 activity as well
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According to this theory the
2019-10-19
According to this theory, the chemical potential of the basic hydrate in the equilibrium condition can be calculated as: , and denote the chemical potentials of the basic hydrate, water and gas, respectively. Also, is the number of gas molecules per water molecules in the basic hydrate. After su
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The desire for COTS products and some potential problems
2019-10-19
The desire for COTS products––and some potential problems There are also technological reasons in support of the use of OTS products. For example, Dawkins and Riddle (2000) point out that the relatively small safety-related systems market cannot sustain the rate of technological advancement stimula
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br Effects of estrogen on
2019-10-19
Effects of estrogen on vascular function Atherosclerosis is a chronic inflammatory condition of the vascular wall (Figure 1) that can be converted to an acute clinical event by the induction of plaque rupture or erosion, leading to thrombosis [58]. This perpetuating process is characterized by ph
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Given that dimethylamine substitution was tolerated as in
2019-10-19
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated RS 127445 HCl amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). Th
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br Materials and methods br
2019-10-19
Materials and methods Results We examined the effects of curcumin in Fluo-4 loaded SH-EP1 IY-5511 kinase stably transfected with human α7-nACh receptor. Application of curcumin alone in the concentrations up to 100 μM for 30 sec. did not induce any detectable change in intracellular Ca2+ leve
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The indigenous populations living at high mountain
2019-10-19
The indigenous populations living at high mountain regions of the Himalayas represent successful human PAI-039 to hypoxia. These populations have undergone selective positive natural selection over millennia across several genomic loci and exhibit unique respiratory, cardiopulmonary and haematologi
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br Rationale and hypothesis To discover an allosteric
2019-10-19
Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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