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Considering their good FAAH inhibitory activity compounds an
2022-08-03

Considering their good FAAH inhibitory activity, compounds and have been selected for an in vivo study in a DSS-induced colitis model. Specific Pathogen Free male 7weeks old C57/Bl6 mice received 2.5% DSS in drinking water during 8days. Concomitantly, they were administrated daily intraperitoneall
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Recent studies are beginning to explore this
2022-08-03

Recent studies are beginning to explore this complex interplay of pathways. For example, intracellular trafficking of poly(lactic-co-glycolic acid)(PLGA) based nanoparticles was studied in detail using 30 different Rab proteins as markers for intracellular transport vesicles (involved in exocytosis,
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br Conclusions Histone acetylation deacetylation is
2022-08-03

Conclusions Histone acetylation/deacetylation is a major epigenetic mechanism implicated in the regulation of transcription and various biological processes such as development and gametogenesis from plants to vertebrates. However, despite being well characterized in zebrafish, acetyltransferase
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br Experimental procedures br Results
2022-08-03

Experimental procedures Results Hdc-KO mice show basal activation of the MAPK and AKT/GSK3β pathways in the dorsal striatum (Rapanelli et al., 2014). These signaling pathways are differentially regulated by the H3 receptor in dMSNs and iMSNs in wild-type mice (Rapanelli et al., 2016). To bette
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The neurotransmitter histamine plays a key role
2022-08-03

The neurotransmitter histamine plays a key role in the sleep-wake cycle and in learning and memory. Alterations in Simeprevir histamine levels are closely connected with central nervous system dysfunction, and are thought to contribute to neurological disorders, including Alzheimer's disease and dep
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To assess the roles of GPR and GPR
2022-08-02

To assess the roles of GPR120 and GPR40 in malignant properties of pancreatic cancer cells, we generated GPR120 and GPR40 knockdown (PANC-sh120 and PANC-sh40, respectively) Thymidine from PANC-1 (Fig. 2A). While no difference of cell growth rate between control PANC-RFP cells and PANC-sh120 cells w
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Based on these findings we set out
2022-08-02

Based on these findings, we set out to identify GPR109A agonists capable of biasing the receptor's signaling towards the functional anti-lipolytic and presumed therapeutic response, and away from the flushing side-effect pathways. Indeed, using recombinantly expressed GPR109A, two classes of compoun
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With this goal in mind we proceeded to explore
2022-08-02

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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First class II fusion proteins are known to
2022-08-02

First, class II fusion proteins are known to transition from a (homo- or hetero-) pre-fusion dimer to a post-fusion trimer [57], [58], [59], [60], [61], [62] through a monomeric intermediate [63], [64], and a crystalline structure of a monomer of Rift Valley fever virus (a phlebovirus, member of the
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PBI is an agonist of GPR and acts as
2022-08-02

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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br Characterization and regional localization of Glu transpo
2022-08-02

Characterization and regional localization of Glu transporters Molecular studies led to the description of five subtypes of plasma membrane Glu transporters termed in accordance to their human or rodent origin (Kanai and Hediger, 1992, Pines et al., 1992, Storck et al., 1992). In humans, these tr
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br Redox regulation in the brain Reactive oxygen species are
2022-08-02

Redox regulation in the brain Reactive oxygen species are generated in α-Cyperone sale by the mitochondrial respiratory chain, which occurs on the inner mitochondrial membrane (Murphy, 2009, Jensen, 1966, Dickinson and Chang, 2011). Interestingly, although most cancer cells are thought to primar
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br Introduction Maintaining blood glucose within
2022-08-02

Introduction Maintaining blood glucose within an appropriate range is crucial for survival. In diabetes, those who suffer episodes of severe hypoglycemia have an increased risk of death [1], [2]. The AH 6809 is especially dependent on an adequate, continuous supply of circulating glucose to fuel
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Recently several dual GLP GIP receptor agonists
2022-08-02

Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously
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br Conflict of interest statement br Introduction br Gap
2022-08-02

Conflict of interest statement Introduction Gap junction assembly Induced disassembly of gap junctions The regulation of connexin and gap junction turnover are still not well understood. This is, in part, due to the fact that while the overall turnover of connexin molecules is fairly con
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