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Overall ABC transporters are hypothesised to prevent the
2022-08-05
Overall, ABC transporters are hypothesised to prevent the penetration of AEDs and other pharmacological compounds into the brain, being a hurdle for therapeutic delivery in neurological diseases. DRE is thought to be in part related to an increased expression of efflux transporters in the BBB, altho
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Optimization of the tetrahydroindazole series led to the dis
2022-08-05
Optimization of the tetrahydroindazole series led to the discovery of two moderately potent γ-secretase modulators, 2-cyclobutane and 2-hydroxy-2-methylpropane which were subsequently evaluated in a kinetic aqueous solubility assay. Unfortunately, neither analog demonstrated improved solubility ().
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Cys loop GABA receptors are well studied
2022-08-05
Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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Through the analysis of various synthetic GPR agonists as re
2022-08-04
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic S-Adenosylhomocysteine receptor motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early pe
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The cases of the Berlin
2022-08-04
The cases of the Berlin and London patients also highlight our limits to defining an HIV cure. No signs of the virus have been found in numerous assays with multiple samples from diverse tissues that Timothy Brown has generously contributed to advance research over the past 12 years. In the case of
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br Memories can last a lifetime long
2022-08-04
Memories can last a lifetime, long after the transient events have passed. The fact that information stored in the bun hot can outlast the environmental trigger implies that enduring cellular changes in the central nervous system underlie memory. Epigenetic modifications of DNA and chromatin stru
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Dual H H receptor antagonists developed by GlaxoSmithKline h
2022-08-04
Dual H1/H3 receptor antagonists developed by GlaxoSmithKline have also reached clinical trials at various stages. These candidates are useful for alleviating the symptoms associated with allergic rhinitis(Daley-Yates et al., 2012). GSK-1004723, 4-[(4-chlorophenyl)methyl]-2-( (2R)-1-[4-(4- [3-(hexahy
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Thus regardless of its specific function PTC
2022-08-04
Thus, regardless of its specific function, PTC52 is associated with plastid activity. During arbuscular mycorrhizal symbiosis, elongated plastids, which are interconnected through thin, tubular plastid projections called stromules, proliferate in arbuscule-containing root cortex cells (Fester et al.
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We also conducted analyses on
2022-08-04
We also conducted analyses on the functional category of UP_Keywords and on KEGG pathways for further understanding. The UP_Keywords analysis (D) demonstrated that acetylation and phosphoprotein were highly enriched categories. KEGG pathways categories (E) of ribosome biogenesis in eukaryotes, DNA r
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A second feature of the
2022-08-04
A second feature of the Ras-type GTPases is that their ‘on’ and ‘off’ states are temporally and often spatially separated from one another. This feature is essential for GTPases mediating signaling and other processes that need to be kept ‘off’ until the arrival of signaling cues. The need to recrui
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This variant has also been related to
2022-08-04
This variant has also been related to a better treatment response in patients with metastatic colorectal cancer subjected to irinotecan-based chemotherapy (Kweekel et al., 2008). Inheritance of this metabolic variability has also been stated to influence better treatment outcomes in breast cancer pa
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Having identified initial leads and further lead optimizatio
2022-08-04
Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic Preladenant synthesis derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, m
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GSK can function in regulating insulin signaling and
2022-08-04
GSK-3 can function in regulating insulin signaling and glucose metabolism. Inactivation of GSK-3 activity results in dephosphorylation and activation of GS that leads to improved glucose tolerance. However, there are additional mechanisms that can lead to increases in GS activity and improve insulin
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Furthermore increased plasma levels of endoglin have been as
2022-08-04
Furthermore, increased plasma levels of endoglin have been associated with diabetic complications (Valbuena-Diez et al., 2012). The involvement of soluble endoglin in a number of widespread pathologies demonstrates that endoglin is not only marker of endothelial integrity but also a causative factor
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br GSK Glycogen synthase kinase GSK is a ubiquitous serine
2022-08-04
GSK-3 Glycogen synthase kinase-3 (GSK-3) is a ubiquitous serine/threonine kinase that is involved in multiple signaling pathways that are crucial for cellular metabolism and proliferation (Doble and Woodgett, 2003, Frame and Cohen, 2001, Grimes and Jope, 2001, Woodgett, 1990). GSK-3 is known to d
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