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br TGR Agonists br FXR TGR Dual
2021-09-27
TGR5 Agonists FXR/TGR5 Dual Agonists In 2010, a FXR/TGR5 dual agonist, 51 (INT-767), was reported [57]. Using an AlphaScreen coactivator recruitment assay, the potency of 51 at FXR was 30nM. In NCI-H716 cells, 51 stimulated intracellular cAMP secretion with an EC50 of 0.63μM. Its TGR5 potency
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RGFP966 Also considered very rare is progressive encephalomy
2021-09-27
Also considered very rare is progressive encephalomyelitis with rigidity and myoclonus (PERM); sometimes called Stiff Person Syndrome Plus (SPS Plus) and with antibodies to glutamic RGFP966 decarboxylase (GAD). However, PERM is now increasingly found with glycine receptor antibodies (GlyR-Ab), in ad
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We confirmed a decrease in extracellular glutamate uptake an
2021-09-27
We confirmed a decrease in extracellular glutamate uptake and the presence of efflux in an endothelial cell model of oxygen-glucose deprivation (OGD), which effectively simulates the inefficient energy supply after brain injury [15], and analysed the function of endothelial EAATs and explored the ro
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Epidemiological evidence indicates that neuroinflammation pl
2021-09-27
Epidemiological evidence indicates that neuroinflammation plays a pivotal role in pathogenesis of AD (Heneka et al., 2015, Heneka et al., 2013, Holmes et al., 2009, Liu et al., 2016). For example, prolonged treatment with nonsteroidal anti-inflammatory drugs reduces the risk of developing AD (In et
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A group of small molecule
2021-09-26
A group of small molecule with a more promising therapeutic mechanism are known as γ-secretase modulators (GSMs), which modulate the cleavage activity of γ-secretase (and likely a host of other substrates) and specifically reduce the levels of the fibrillogenic Aβ42 peptide without altering the ε-si
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To date types of glucose
2021-09-26
To date, 14 types of glucose transport protein have been discovered, each having its own specific functions with different distributions [33]. Among these, GLUT4 is particularly important for maintaining glucose metabolism homeostasis and insulin sensitivity, since it is involved in glucose transpor
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Galanin was shown to play an important
2021-09-26
Galanin was shown to play an important role in pain and pain processing [14] and the involvement of neuropeptides in the development of migraine is well established [[24], [25], [26]], however, so far it has not been examined whether systemic galanin levels correlate with migraine. Therefore, we use
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br Summary br Conflict of interest br
2021-09-26
Summary Conflict of interest Acknowledgments This study was supported by Grant No. 2014/13/B/NZ7/02277 from the National Science Centre, Poland. Introduction Progesterone (P) is an anticonvulsant hormone (Backstrom et al., 1984, Herzog, 1995, Herzog, 1999, Frye et al., 2000, Reddy, 2002
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DIS used standard methods for locating and contacting person
2021-09-26
DIS used standard methods for locating and contacting persons for interview, including the use of phone calls, letters, in person contact, and contact through social media. During this time period, contacts of persons with diagnosed HIV (first-generation contacts) were tested for HIV and, regardless
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NPxY was recognized as the
2021-09-24
NPxY was recognized as the first short signal sequence motif in the cytoplasmic domain of membrane receptors and proteins with critical roles in internalization and trafficking of receptor molecules [130]. Including LDL receptor, beta-1 integrin, megalin, beta-amyloid precursor protein, EGF receptor
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br Glycoengineering br The Omics perspective
2021-09-24
Glycoengineering The « Omics » perspective The publication of the CHO-K1 genome sequence in 2011, followed by the publication of two Chinese hamster and six CHO cell line genomes in 2013, bring new opportunities in developing and engineering CHO h89 for improved glycoprotein production (Xu et
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The current study also inferred
2021-09-24
The current study also inferred that MT content in Crassostrea gigas might be associated with the Cd level, and can be affected by MT turnover. The Boc-D-FMK synthesis of MT in cytosol is beneficial for aquatic organisms to adapt the seawater contaminated by heavy metals, and MT is a biomarker for
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br Evasion strategies for enhanced therapeutic
2021-09-24
Evasion strategies for enhanced therapeutic outcomes In order to increase AED penetration into the CNS, several strategies have been developed over the years to overcome the activity of efflux transporters, by inhibiting their function or by regulating their expression. Due to the high relevance
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Cefepime Dihydrochloride Monohydrate depicts the synthesis o
2021-09-24
depicts the synthesis of series with a four-step sequence. First, the commercially available 4-hydroxybenzaldehyde () was condensed with 2-bromoethanol through Mitsunobu reaction to give the key intermediate (). Next, conventional nucleophilic substitution reaction with the privileged structures (
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Acknowledgments The authors would like to thank members of t
2021-09-24
Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD
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