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br Methods br Results We have previously used hex
2022-03-23

Methods Results We have previously used ß-hex assays in HeLa Tioconazole sale to study the role of lysosomal exocytosis on transition metal clearance and the effects of transition metals on lysosomal exocytosis [26], [29], [40]. ß-hex is a lysosomal enzyme, the delivery of which to the extrac
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The importance of the histone chaperone function of Hat p
2022-03-23

The importance of the histone chaperone function of Hat1p was highlighted by the recent demonstration that the catalytic activity of Hat1p is not sufficient for its function in vivo. Fusion of a nuclear export signal (NES) to yeast Hat1p effectively excluded the enzyme from the nucleus, with a conco
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The other possibility for the lack of effects
2022-03-23

The other possibility for the lack of effects of H1 receptor agonists, e.g. histamine, on the NMDAR-mediated responses is that other neurotransmitters may cause more profound effects than histamine on the gliotransmitter release from astrocytes. For example, recent studies showed that noradrenaline,
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Evidence indicates that astrocytes play a role in
2022-03-23

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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The molecular mechanism of gliotransmitter release is
2022-03-23

The molecular mechanism of gliotransmitter release is not fully understood until now, and previous studies have emphasized that the elevation of [Ca2+]i triggers vesicular Copanlisib of glutamate. Parpura et al. reported that the essential role of Ca2+ release from internal stores in glutamate rele
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Reduction of the hydrolysis of ATP is
2022-03-23

Reduction of the hydrolysis of ATP is an important strategy to reduce ischemia/reperfusion injury. Increased intracellular concentrations of solutes secondary to ATP depletion are known to result in osmotic swelling that may be sufficient to cause sarcolemmal rupture. Cinaciguat activates sGC direct
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br All platelet agonists acting through specific
2022-03-23

All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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The absolute requirement for substrate prephosphorylation ra
2022-03-23

The absolute requirement for substrate prephosphorylation raised the possibility that short phosphorylated peptides might serve as selective substrate competitive inhibitors. A set of phosphorylated peptides patterned after known GSK-3 substrates was generated and shown to inhibit GSK-3 in vitro in
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While the specific set of challenges associated with
2022-03-23

While the specific set of challenges associated with deorphanization and transforming each poorly characterized GPCR into a useful drug target will be unique, much can be learned by considering how these issues have been addressed for other receptors. One group of poorly characterized GPCRs that hav
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Finally our work showed that HAART resulted in significant i
2022-03-23

Finally, our work showed that HAART resulted in significant inter-individual variability among DEGs, which reflected the 3787 receptor in HIV-affected human gene expressions (Fig. 1, Fig. 2, Fig. 3, Fig. 4). These observations also highlighted the importance of determining common as well as persona
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The compounds described in this paper
2022-03-22

The compounds described in this paper were prepared using a modular approach that allowed diversification of R or R at the final step (). Route A involved amide coupling of -butyl 4-(methylamino)piperidine-1-carboxylate with phenyl acetic acids (step a) using 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-m
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SAR around amino derivative revealed a number of
2022-03-22

SAR around amino-derivative revealed a number of interesting trends related to the serum shift and in vitro activity (). A comparison of derivative , and its epimer , showed that the stereochemistry had little effect on the serum shift and the intrinsic affinity for the receptor. In contrast, re-p
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Similar to GPR A activation
2022-03-22

Similar to GPR109A, activation of G-protein-coupled receptor 81 (GPR81, also called HCAR1 (hydroxycarboxylic neomycin sulfate receptor 1)) by lactate suppresses lipolysis (Fig. 1), suggesting GPR81 to be a potential drug target for treating T2DM (Boyd et al., 1974, Cai et al., 2008, Gold et al., 196
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The expression of heat shock proteins HSPs can
2022-03-22

The expression of heat-shock proteins (HSPs) can be upregulated by viral infection, nutritional deficiency, TNF-α and oxidative stress in Paeonol [44], [45] HSPs are classified in six families (including the HSP10, HSP40, HSP60, HSP70, HSP90 and HSP100 families). HSP90 [46] for example provides a na
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In addition to vertebrate species GnRH has been identified
2022-03-22

In addition to vertebrate species, GnRH has been identified in invertebrates, such as in the Protochordate Ciona intestinalis (Powell et al., 1996; Adams et al., 2003), the decapods mollusk Octopus vulgaris (Iwakoshi et al., 2002), the gastropod mollusk, the sea hare Aplysia californica (Zhang et al
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