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br Materials and methods br Results br Discussion
2022-04-15

Materials and methods Results Discussion Defective regulation and inappropriate activation of the HH signaling pathway is implicated in many cancers. SMO targeting inhibitors were the first to enter clinical trials, however complications with acquired resistance and toxicity, also exemplifi
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To improve the preferential GalR binding we synthesized
2022-04-15

To improve the preferential GalR2 binding, we synthesized M1152 where the N-terminal Gly residue was deleted, in analogy with previously designed M871 (Sollenberg et al., 2006). In addition to the poor affinity of M871 for GalR1, a recent study showed that it also hardly recognized by GalR3 (Sollenb
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br Results and discussion br Conclusion In normal and curd
2022-04-15

Results and discussion Conclusion In normal and curd coconuts, full-length cDNA and parental genomic DNA sequences encoding endosperm specific AGal were sequenced and characterized. At least, three mutation ochratoxin a were identified in CnAGal gene. In vitro expression in K. phaffii showed
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Based on the previous report that FXR regulated PEPCK
2022-04-15

Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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br Results and discussion br Conclusion In summary
2022-04-15

Results and discussion Conclusion In summary, we designed and discovered a series of novel GPR40 agonists containing 3,5-dimethylisoxazole with improved tPSA and ideal cLog P. Most of these compounds were confirmed as excellent GPR40 agonists in vitro. Especially, compound 11k exhibited robust
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Our paper also contributes to the
2022-04-15

Our paper also contributes to the large, but hitherto inconclusive literature that studies the effects of option-based compensation or convexity in compensation on corporate risk-taking policies. On the one hand, some studies document a positive relationship by showing that convexity increases lever
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UM171 synthesis Introduction of a chloropyridine group onto
2022-04-15

Introduction of a chloropyridine group onto the fluoro derivative (→) leads to a similarly potent compound that exhibits a lower /, and as was observed with (), was rapidly cleared. However, the high clearance of () did not prevent the increase in the concentrations of FAAs even as its plasma levels
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In the CNS histamine is known to regulate sleep and
2022-04-15

In the CNS, H-9 dihydrochloride mg is known to regulate sleep and wakefulness, learning and memory, feeding, and energy. Here, we address its actions in relation to CNS disorders, and emphasize potential clinical applications of histamine receptor ligands (Table 1). In addition, as the effect of hi
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Evidence indicates that astrocytes play a role in
2022-04-15

Evidence indicates that astrocytes play a role in the modulation of NMDAR activity in the CA1 (Henneberger et al., 2010; Papouin et al., 2017a, Papouin et al., 2017b; Robin et al., 2018). Therefore, we sought to examine whether astrocytes are involved in the H1 receptor antagonist/inverse agonist-in
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Parkinson s disease is another neurodegenerative
2022-04-15

Parkinson's disease is another neurodegenerative disorder affecting H3Rs. The most common clinical symptoms of this disease are rigidity, bradykinesia, rest tremor, loss of postural reflexes, and gain impairment owing to progressive degeneration of the dopaminergic neurons in the nigro-striatal neur
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br Structural studies of GCAP Recoverin
2022-04-14

Structural studies of GCAP Recoverin was the first member of this subfamily of Ca2+-binding L-Cysteinesulfinic acid to be investigated by structural methods [27], [54], [55], [56], [57], [58]. These proteins have four EF-hands arranged in pairs that give rise to amino- and carboxyl-terminal domai
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br Introduction Excitatory pyramidal neurons are generated i
2022-04-14

Introduction Excitatory pyramidal neurons are generated in the cortical ventricular zone and migrate into the cortical plate alongside the radial glial processes (Chanas-Sacre et al., 2000, Hartfuss et al., 2001, Noctor et al., 2001, Rakic, 1972, Tan et al., 1998). Neuronal migration determines t
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Throughout our studies we used CBD
2022-04-14

Throughout our studies we used CBD under the assumption that it binds to the GPR55 receptor and has antagonist properties at the GPR55 receptor, as previously suggested (Whyte et al., 2009). To clarify whether the GPR55 receptor is involved in the O-1602-mediated effects on GI motility, we performed
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The recently de orphaned G
2022-04-14

The recently de-orphaned G-protein coupled receptor (GPCR), GPR55, is activated endogenously by L-α-lysophosphatidylinositol (LPI), a lipid signaling molecule, as well as N-arachidonoyl glycine (NAGly) and numerous endo, phyto, and synthetic cannabinoids (Oka et al., 2007, Henstridge et al., 2010, H
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Introduction Nicotinic acid niacin NA has
2022-04-14

Introduction Nicotinic b 35 (niacin, NA) has been used in the treatment of dislipidemia and cardiovascular disease for almost 60years (Offermanns, 2006). Large clinical studies showed that niacin alone or in combination with LDL-lowering drugs improved cardiovascular outcomes (Canner et al., 1986,
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