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br Results br Discussion In this study six
2022-04-02

Results Discussion In this study, six new T30695 variants were synthesized with the acyclic R or S glycerol linker instead of DAMGO receptor unit at 4, 8 or 12 T residue. Based on our previous studies on TBA-GQ, this type of modification should provoke local changes in GQ conformations in the
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Compound a substituted phenyl H pyrano d d dipyrimidine deri
2022-04-02

Compound 6, a 5-(4-substituted-phenyl)-5H-pyrano[2,3-d:-6,5-d′]dipyrimidine derivative was invented previously to have significant efficacy to inhibit HIV integrase enzyme with 0.9 ± 0.4 μM of IC50 against 3′-processing and 16.1 ± 10.7 μM of IC50 against strand transfer suppression. The compound ind
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The H R antagonist cimetidine Tagamet
2022-04-02

The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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Ch 55 Expression of p NTR has been linked to several aspects
2022-04-02

Expression of p75NTR has been linked to several aspects of aggressive glioma growth, including migration and invasion, by various mechanisms in a large number of elegant studies [6], [7], [26], [27]. Our study adds to this literature by demonstrating specific roles in hypoxic tumor cells and regulat
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br Materials and methods br
2022-04-02

Materials and methods Author contributions Acknowledgments We thank members of the Skaar laboratory for critical evaluation of the manuscript. This work was supported by grants from the National Institutes of Health, R01AI069233 (EPS), and T32GM008554-21 (LJL). Introduction Pseudomonas
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Numerous strategies of cardiomyocyte protection
2022-04-02

Numerous strategies of cardiomyocyte protection are effective in preclinical, animal models and in small clinical trials. However, most have disappointed in large clinical trials [4,5]. Failures of cyclosporine and post-conditioning to mitigate reperfusion injury are recent examples [[6], [7], [8]].
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carbenoxolone br Brief overview of GSK inhibitors We will br
2022-04-02

Brief overview of GSK-3 inhibitors We will briefly summarize some of the key aspects about GSK-3 inhibitors. Additional details of GSK-3 inhibitors in clinical trials have been recently reviewed [5]. GSK-3 is a complicated target as it is involved in many biological processes from neurology, diab
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AS 101 br Conclusion and future perspectives The nicotinic
2022-04-02

Conclusion and future perspectives The nicotinic AS 101 receptor GPR109A and its close relatives GPR109B and GPR81 are primarily expressed in adipocytes and are coupled to Gi-type G proteins. Recently, the ketone body β-hydroxy-butyrate, the β-oxidation intermediate 3-hydroxy octanoic acid and la
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Abn CBD induced changes reduced microglial cell density cell
2022-04-02

Abn-CBD induced changes (reduced microglial cell density, PSB 0777 ammonium salt size and a lower density of ramification) in the microglial morphology that could be compatible with a blockade of the neuroinflammation provoked by MPTPp. The absence of GPR55 transcripts in microglial cells in striat
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To test our refinement protocol we considered a benchmark se
2022-04-01

To test our refinement protocol, we considered a benchmark set of 12 N-linked glycan-containing protein structures determined by X-ray crystallography at resolutions ranging between 1.9 Å and 3.5 Å and comprising a total of 133 glycan units. We identified four incorrect anomeric configurations and 2
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Regarding the causative diseases of
2022-04-01

Regarding the causative diseases of ES, patients with unknown cause and those with encephalitis had significantly higher CSF levels of energy metabolism of cells against GluN2B-NT2 and GluN2B-CT than the disease controls, but patients with genetic disorder and those with cortical dysplasia showed n
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Due to its unusually long pre implantation
2022-04-01

Due to its unusually long pre-implantation period [20,21], the horse conceptus is entirely dependent on histotrophic nutrition for the first 40 days of gestation [22]. During the pre-implantation period, glucose transporters in the endometrium and conceptus membranes must deliver the glucose require
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br Summary br Acknowledgement br GR A
2022-04-01

Summary Acknowledgement GR: A Nuclear Receptor with Widespread Physiological Impact GR, or NR3C1 (see Glossary), is a transcription factor (TF) that regulates gene expression in nearly every cell of the body. A member of the nuclear receptor (NR) superfamily, its ligand-binding domain confe
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br Materials and methods br Results br
2022-04-01

Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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More recently Dal Peraro and coworkers carried
2022-04-01

More recently, Dal Peraro and coworkers [38] carried out 4 μs CG MD simulations of GS with six randomly placed C9915-55 peptides embedded into a synaptic plasma bilayer model. This lipid raft model was constituted by 32 different serine protease inhibitor and cholesterol (54.74%). In this study, th
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