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Sodium Aescinate synthesis Previously we had proposed three
2019-11-21
Previously we had proposed three possible models, with one being that hCrm1 fundamentally interacted more favorably or strongly with Rev-RRE complex, compared to mCrm1. We decided to test that model, which was the simplest and most straightforward, by both biochemical and genetic means. By using bac
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In recent years there has been much
2019-11-20
In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might also
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Our previous high throughput screening HTS campaign
2019-11-20
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based AMI-1 mg assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [23],
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br Experimental Procedures br Author Contributions br Acknow
2019-11-20
Experimental Procedures Author Contributions Acknowledgments Introduction Oxysterols came to prominence in the late 1970\'s with the oxysterol hypothesis which proposed that the suppressive effect of cholesterol on its own synthesis is mediated through oxysterols not by cholesterol itsel
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Of the acidic hydroxyazoles involved hydroxypyrazole had the
2019-11-20
Of the acidic hydroxyazoles involved, hydroxypyrazole had the weakest acidic profile (pKa in the range of 6–7), although highly deprotonated at physiological pH. During hit optimization, the two pyrazole ring positions available for substitution provide an opportunity for a better exploration of the
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Therefore in this study we determined whether exogenous LTD
2019-11-20
Therefore, in this study we determined whether exogenous LTD, a potent agonist of both CysLT and CysLT receptors , , induces MRS 2578 edema and AQP4 expression in mouse brain; if so, which subtype of the receptors is involved in AQP4 expression in mouse brain and the cultured rat astrocytes. Mate
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Published results have revealed relationships between serine
2019-11-20
Published results have revealed relationships between serine 81 in AR and some CDKs, especially CDKs 1, 5 and 9 [12], [13], [14], [15], [16]. These results are often supported by pharmacological inhibition of a certain CDK. An effect of CDK1 inhibition on suppression of S81-phosphorylation was previ
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Although the implication of DA and glutamate signaling cross
2019-11-20
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement
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br Marginal zone lymphoma Marginal
2019-11-19
Marginal zone lymphoma Marginal zone lymphoma (MZL) comprises three lymphoma entities that arise from the marginal zone surrounding the germinal center: extranodal MZL or mucosa-associated lymphoid tissue (MALT), splenic MZL, and nodal MZL. Deep sequencing of nodal MZL patients found that 5/35 (1
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Some pyrimidine analogs are substrate based inhibitors that
2019-11-19
Some pyrimidine analogs are substrate-based inhibitors that bind to the dihydroorotate binding site, but most reported inhibitors of DHODH bind to the site occupied by the ubiquinone co-factor., , , , , , , , , , , , , , , , , X-ray crystallographic studies of inhibitor complexes with DHODH and DHO
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Altogether we have shown the presence
2019-11-19
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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Given the importance of cysteine cathepsin inhibitors as put
2019-11-19
Given the importance of cysteine cathepsin inhibitors as putative therapeutic molecules and microbial virulence factors, we chose to investigate whether Yersinia enterocolitica may be a potent producer of such inhibitors. Y. enterocolitica is the most heterogeneous species within the genus Yersinia.
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Autophagy is a dynamic process that primarily
2019-11-19
Autophagy is a dynamic process that primarily involves autophagosome formatting and lysosomal degradation, and these processes are controlled by autophagy-related genes (Atg) (Klionsky et al., 2012). The related protein SQSTM1/p62 (sequestosome 1) importantly serves as a signalling director in sever
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In the frontal cortex the present
2019-11-19
In the frontal cortex, the present study found a relationship between working memory performance and activated Erk2 expression for the E2-only group, where animals that tended to perform better on the WMC measure tended to have higher activated Erk2 expression. This suggests that there is a unique r
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Memantine hydrochloride Additionally both in vitro and in vi
2019-11-19
Additionally, both in vitro and in vivo studies showed that a Ca2+ influx is closely related to apoptosis (Rizzuto et al., 2003). Calmodulin (CaM) is a multifunctional intermediate calcium-binding messenger protein expressed in all eukaryotic cells, which senses intracellular calcium levels by bindi
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