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This structure guided the variation of the compounds
2020-05-06
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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The mechanisms in the central nervous system CNS
2020-05-06
The mechanisms in the central nervous system (CNS) controlling the sympathetic tone of the ABC294640 are associated to behavioral strategies, such as those involved in response to stress. In this regard, morphine withdrawal induces profound and severe stress reactions evidenced by enhancement of NA
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Epitope analyses of AT AA
2020-05-06
Epitope analyses of AT1-AA and ET-AA indicate that the Exendin-3 (9-39) amide of both autoantibodies are located at the second extracelluar loop of both receptors. The specific epitopes for both autoantibodies are similar to what was reported previously in a cohort of patients from Brazil [6] and f
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To provide a brief critical evaluation
2020-05-06
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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CXCR is not only critical in the B cell
2020-05-06
CXCR5 is not only critical in the B cell lineage in FL. A high proportion of CXCR5-expressing follicular helper T cells (TFH) were observed in FL but not in closely related DLBCL [141] and further investigation revealed that FL regulatory T cells (Tregs) used a CXCL13-CXCR5 autocrine loop for positi
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Ginsenoside Re lysine mixture had increased anticancer effec
2020-05-06
Ginsenoside Re-lysine mixture had increased anticancer effects upon heat processing by regulating Bcl-2 and Bax (Yamabe et al., 2013). Ginsenoside Re (20mg/kg) inhibited NF-κB activation by inhibiting LPS binding to TLR4 on macrophages in TNBS-treated mice (Lee, Hyam, Jang, Han, & Kim, 2012). The ch
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The aniline R group was extensively explored and
2020-05-05
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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Although several examples of selective reduction of diazoest
2020-05-05
Although several examples of selective NPS-2143 receptor of α-diazoesters to α-hydrazonoesters have been described in the literature, reports on practical and general examples of such a process are scarce. In this context, there was a need to devise a mild and general method for the selective reduc
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br Material and methods br Results Diagrammatic representati
2020-05-05
Material and methods Results Diagrammatic representations showing the bilateral injection sites in the BNST of all animals used in the present study are presented in Fig. 1. Discussion The present results provide the first evidence that both CRF1 and CRF2 receptors in the BSNT are involved
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The present results are potentially relevant for
2020-05-05
The present results are potentially relevant for understanding anxiety disorders and their treatment. Both COMT Val158Met (Lonsdorf and Kalisch, 2011, Montag et al., 2012) and neuroticism/anxiety (Clark et al., 1994, Mineka et al., 1998, Weinstock and Whisman, 2006) have been linked to the prevalenc
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br Results and discussion br Conclusion This study describes
2020-05-05
Results and discussion Conclusion This study describes the development of a highly sensitive on-sorbent derivatisation technique, using the novel high-surface area CMV devices, to sample methamphetamine vapour. Previous methods for air sampling for methamphetamine such as sampling cassettes ha
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br Experimental br Declaration of interest br Introduction b
2020-05-05
Experimental Declaration of interest Introduction Material and methods Results and discussion Conclusion By screening the NMR Hyper Assembly Cloning library an initial hit was found for an inhibitor of the PPI between the α-β subunits of CK2 with an IC50 of 900 μM. This compound wa
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br Experimental procedures br Results
2020-05-05
Experimental procedures Results Fluorescence attributable to GnRH-eGFP neurons was observed through the diagonal band of Broca, to the POA of the hypothalamus in GnRH-eGFP transgenic rats for all groups as described previously (Kato et al., 2003, Tada et al., 2013). Discussion The mEPSCs w
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Addition of deoxyuridine to CY cultures led to
2020-05-05
Addition of deoxyuridine to CY11 cultures led to a significant decline in the amount of uracil-DNA (Fig. 5). Deoxyuridine effectively induces the deo operon and is efficiently degraded to uracil and deoxyribose 1-phosphate by the deoA gene product, thymidine phosphorylase; a minor percentage of deox
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Additionally although the membrane localized ER signaling de
2020-05-05
Additionally, although the membrane-localized ER signaling described in this review has generally been studied in isolation from nuclear signaling, it is becoming clearer and clearer that integration of these mechanisms must be considered (Frick, 2015). Perhaps the distinct estradiol signaling mecha
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