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The compounds described in this paper
2022-04-26
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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br GPR is a class
2022-04-26
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine SAR 405 which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-cell sign
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We hypothesized that modulating redox stress
2022-04-26
We hypothesized that modulating redox stress by altering endogenous antioxidant content (overexpression of catalase) and/or via dietary intervention will improve energy metabolism, adipose tissue function, and overall glucose and lipid homeostasis. To better understand the interplay between redox re
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In addition to redox stress nutritional intake plays
2022-04-26
In addition to redox stress, nutritional intake plays a key role in modulating energy metabolism. DIO animal models are commonly used to study altered metabolic changes consequential to fat storage within various fat pads. In general, diets containing >40% high-fat lard, milk, and butter promote exc
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The pharmacokinetics of was obtained
2022-04-26
The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indi
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Fmoc-Phe-OPfp br Next we explored the SAR
2022-04-26
Next, we explored the SAR around the aryl ring attached to the pyrrole nitrogen in the presence of the 3-CF and the 2,6-difluorophenylpropionic Fmoc-Phe-OPfp sidechain (). The EC value of the unsubstituted phenyl was about 100 nM. The 4-methyl was 2-fold more potent, however ethyl and bromo did no
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br Conclusion br Acknowledgements This
2022-04-26
Conclusion Acknowledgements This work was supported by a Grant-in-Aid for challenging Exploratory Research (15K12715) and was a partly supported by Suzuken Memorial Foundation (2014). The authors would like to thank Enago (www.enago.jp) for the English language review. G protein-coupled rec
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br Materials and methods br
2022-04-26
Materials and methods Results Discussion Previously, it is well known that methionine and choline deficient (MCDD) or choline-deficient, L-amino acid-defined (CDAA) models are widely accepted in NASH research. MCDD or CDAA dietary model has been mimic human NASH in rodents by sequentially p
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Molecular mechanisms of decidualization have been studied
2022-04-26
Molecular mechanisms of decidualization have been studied for years, revealing numerous signaling pathways and transcriptional factors participated in the regulation [37,38]. As a central controller of deicdualization, FOXO1 regulates the transcription of a large number of target genes, which are in
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In addition researchers studying GPR agonists favor
2022-04-26
In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it Fmoc-Thr(tBu)-OH is unclear why Sanofi-Aventis chose to terminate collaboration with Met
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Based on the results of compound appeared to have
2022-04-26
Based on the results of , p-Cresyl sulfate australia appeared to have the best overall profile, so our efforts were then devoted to using 5-(-propyl)pyrimidine as the right-hand nitrogen attachment to optimize the R group of (). Analog was synthesized using the reaction conditions from , while anal
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Disrupting the dialog between microbiota and the host especi
2022-04-26
Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated
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SB 203580 Treatment with probiotics can also
2022-04-26
Treatment with probiotics can also be used to alter the microbiota profile of CF patients. One study reports that administration of the probiotic Lactobacillus Reuteri improved digestive health and inflammation [112]. The fecal microbial profile changed, showing a decrease in Proteobacteria and an i
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Dendritic damage and loss of synaptic connections
2022-04-26
Dendritic damage and loss of synaptic connections correlate with cognitive decline in HAND patients. Synapse loss induced by HIV proteins occurs early and via a different signaling pathway from that leading to neuronal death (Kim et al., 2008), suggesting that synapse loss might be a mechanism to re
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br Concluding remarks br Introduction The hair cells of
2022-04-25
Concluding remarks Introduction The hair PFI-2 mg of vestibular organs detect linear and rotational head movements, providing sensory information that is essential for normal postural and visual reflexes. Most vestibular hair cells are produced during embryonic development, but they can be lo
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