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To apply the recently developed GPR ligands
2022-05-13
To apply the recently developed GPR35 ligands to CNS disorders, it is necessary to understand whether GPR35 is expressed by any identified cell types in the AZ20 and whether activation or blockade of this receptor has any consequence on the activity of the neuronal circuitry. To this end, the prese
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BAY 61-3606 receptor br Surrogate ligands for GPR Although i
2022-05-13
Surrogate ligands for GPR35 Although identification of endogenously produced chemicals with agonist action at GPR35 is of considerable importance, the ligands described above are far from ideal to probe the roles of GPR35. Surrogate ligands are therefore required. Until recently, the key GPR35 ag
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In summary through medicinal chemistry
2022-05-13
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on
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br Results br Discussion Cell contact mediated spread
2022-05-13
Results Discussion Cell-contact-mediated spread of HIV-1 has been estimated to be at least an order of magnitude more efficient compared to passive dissemination of particles through the extracellular milieu. Thus, this form of viral transmission can have significant effects on the pathogenesi
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In conclusion we provided the first evidence
2022-05-13
In conclusion, we provided the first evidence of a modification and regulation of GCK by O-GlcNAc modification that until now was not explored. This discovery provides important clues in the prevention of hyperglycemia and development of novel therapeutic drugs to treat type 2 diabetes. Acknowled
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SH-4-54 The OTR and GHSR are known to play similar
2022-05-13
The OTR and GHSR are known to play similar roles in centrally regulated behaviours, where the OTR is implicated in mood, sociability and appetite regulation (Morton et al., 2012; Myers et al., 2014; Sala et al., 2013; Lukas et al., 2011; Slattery and Neumann, 2010), with the GHSR primarily involved
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For the two KO models CX and
2022-05-13
For the two KO models (CX30 and CX43), fluorescence recovery is almost always best fitted with a 2-component exponential (Fig. 6A and D). Statistical analysis of the parameters (Table 1) shows that in both cases the two time scales and the fraction of recovery associated with the fast intracellular
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Primarily because secretase was a therapeutic target in AD
2022-05-12
Primarily because γ-secretase was a therapeutic target in AD, a plethora of γ-secretase inhibitors (GSIs) have been developed that effectively inhibit γ-secretase cleavage in humans [16]. Indeed, “druggability” of γ-secretase has not been an issue even when the identity of the target was unknown in
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Ebastine australia br Galanin in depression A major impedime
2022-05-12
Galanin in depression A major impediment in depression research is the lack of validated animals´ models. Animals not only lack consciousness of self, self-reflection and consideration of others but also hallmarks of the disorder such as depressed mood, low self-esteem or suicidal intent are hard
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Fibroblast growth factor receptors FGFRs play an essential
2022-05-12
Fibroblast growth factor receptors (FGFRs) play an essential role in the regulation of cell survival, proliferation, migration and differentiation. FGFRs are a family of receptor tyrosine kinases (RTKs) exhibiting an extracellular immunoglobulin (Ig)-like ligand binding domain, a transmembrane domai
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In conclusion the present study shows that the endothelin
2022-05-12
In conclusion, the present study shows that the endothelin system is of importance in the cardiopulmonary vascular pathophysiology of porcine endotoxin shock. In this model, combination of a selective endothelin ETA and a selective endothelin ETB receptor antagonist markedly improved pulmonary circu
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br Materials and methods br Results br Discussion Several
2022-05-12
Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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This crosstalk may be responsible for the beneficial effects
2022-05-12
This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on opioid receptor antagonist pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of
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In the same research group released a free internet accessib
2022-05-12
In 2017, the same research group released a free internet accessible database (HemeOxDB, http://www.researchdsf.unict.it/hemeoxdb), to make it easier the analysis of the literature and, consequently, the design of potent and selective HO-1 inhibitors. The database reported the entire set of HO-1 and
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br Conclusion Whilst acknowledging that forensic science cri
2022-05-12
Conclusion Whilst acknowledging that forensic science critically needs strategic investment across every domain [27], forensic science needs to bring both ‘hedgehog’ and ‘fox’ approaches together to address the roots of the major challenges the discipline faces. Addressing these challenges in a w
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