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As disclosed in our preceding paper medicinal chemistry
2021-12-02
As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, 5(S),6(R)-7-trihydro
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br Regulation of Glu transporters
2021-12-02
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino Gastrodin calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These include transcripti
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br Involvement of gap junctions and Panx in
2021-12-01
Involvement of gap junctions and Panx1 in spinal cord processing of pain information Several studies indicated that GJs in the CNS contribute to pain. A common finding in such studies is that intrathecal administration of GJ blocker attenuates pain behavior. For example, intrathecal CBX attenuate
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The Notch cleavage efficiency of Aph
2021-12-01
The Notch-cleavage efficiency of Aph1aS containing complexes was lower than that of Aph1aL γ-secretases, especially in combination with PS2, suggesting that Aph1aS is a determinant of low Notch-cleavage specificity, considering that the different subcellular localization of PS1 and PS2 didn't affect
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No G C pattern managed
2021-12-01
No G4C pattern managed to capture all GQ forming sequences of the reference dataset. The sequences that were missed by even the most flexible models were AGATGGAGTGGAGAGG, AGGAGATGCAGGAG, AGAGGGTAGATGG and TTTTTAAAAGAAGGGGAGGAATAGGGGATATGA. In fact, the former three are not expected to form any unim
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A breakthrough in the understanding
2021-12-01
A breakthrough in the understanding of the unique properties of GPX4-downregulation-induced cell death was accomplished when Seiler et al. in 2008 demonstrated the role of 12/15-lipoxygenase (12/15-LOX), a polyunsaturated fatty Nexturastat A australia metabolizing enzyme [92], in the execution of GP
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m6A Another important question for future
2021-12-01
Another important question for future studies will be whether FAAH inhibitors work to normalize impairments in fear extinction that are known to be produced by environmental insults such as exposure to abused drugs and stress 97, 103. Indeed, several authors have posited utility of FAAH inhibitors f
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br Effects of norepinephrine on HIV
2021-12-01
Effects of norepinephrine on HIV infection The few in vitro studies specifically examining the effects of norepinephrine on HIV infection suggest that this catecholamine can influence the HIV replication process, although the precise mechanism is unclear. Cole and colleagues found concentrations
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br Acknowledgments This study was financially supported by
2021-12-01
Acknowledgments This study was financially supported by National Science Center Poland grant No DEC-2011/02/A/NZ4/00031 (KKK), Jagiellonian University Medical College (Poland) grants: K/ZDS/007130 (SM) and K/ZDS/007131 (SM), COST Action CA15135 (DŁ, HS, KKK) and DFG INST 208/664-1 FUGG (HS). Than
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The central region of Azalanstat can be substituted with con
2021-12-01
The central region of Azalanstat can be substituted with connecting alkyl chains of different nature and length. Interesting results were given by compounds with a four or five AMD-070 chain, incorporating heteroatoms, such as oxygen (Fig. 2, compound 4) or sulfur, and different functional groups s
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Cytochalasin J To identify factors associated with
2021-12-01
To identify factors associated with being HCV-unaware, univariable and multivariable logistic model were used, odds ratios, 95% confidence intervals and p-values were reported. We included in the multivariable model factors associated with unawareness of HCV infection in univariable analysis with a
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We did however observe that niacin treatment impaired DC acc
2021-12-01
We did, however, observe that niacin treatment impaired DC accumulation in skin-draining lymph nodes (Fig. 2). Attenuated adaptive immunity, assessed using a contact hypersensitivity assay (Fig. 4), was observed, as would be expected from impaired DC accumulation in lymph nodes, though other mechani
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br Several reports have shown an anti proliferative effect o
2021-12-01
Several reports have shown an anti-proliferative effect of type I IFNs on CD4+ T NVP-TAE684 australia activated in vitro either upon anti-CD3 antibody treatment [28,29] or upon cognate antigen stimulation [29]. However, the in vivo setting is a lot more complex, since the final outcome is the net
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So far the functional significance of GluR A and GluR
2021-11-30
So far, the functional significance of GluR-A and GluR-B in synaptic plasticity has been best studied in the context of long-term potentiation of synaptic transmission in vitro in the hippocampus and the regulation of synaptic strength in paradigms underlying activity-dependent learning in vivo Taka
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Hypocotyl development is a crucial phase of early vegetative
2021-11-30
Hypocotyl development is a crucial phase of early vegetative growth that influences seedling vigor contributing to fitness and productivity of a plant system (Stinchcombe and Schmitt, 2006; Luo et al., 2017). The development of a hypocotyl is characterized by an initial slow growth phase followed by
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