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For some agonists these stable GPR responses
2022-01-14
For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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br Introduction High dose niacin
2022-01-14
Introduction High dose niacin, or nicotinic acid, has been used as an athero-protective drug for more than 50 years (Carlson, 2005, Offermanns, 2006). When taken in pharmacological doses (>1g/day), the nicotinic Y-27632 form of niacin modulates plasma lipid profiles including decreasing circulat
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mitotic inhibitor br Conclusion br Author statement br Ackno
2022-01-14
Conclusion Author statement Acknowledgments Introduction The hypothalamic-pituitary-gonadal (HPG) axis is an important neurohormone network for vertebrates that regulates their gonadal development and maturation, guarantees their pubertal development and maintains their normal reproducti
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No compounds in this series showed any appreciable activity
2022-01-14
No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in mal
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Neurotransmitter transporters are rapidly recycled from and
2022-01-14
Neurotransmitter transporters are rapidly recycled from and to the membrane. For instance, the GABA transporter GAT1 is recycled in a calcium and depolarization dependent manner. GAT1 located in the plasma membrane is internalized to a subpopulation of small vesicles different from the classical neu
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Peripheral injury or disease induced alterations in synaptic
2022-01-14
Peripheral injury- or disease-induced alterations in synaptic efficacy occur not only at the first synapse made by the primary nociceptive afferents in the spinal dorsal horn but are also operational in several regions processing the sensorimotor as well as emotional-affective components of pain, su
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Underlying this study is the hypothesized importance of
2022-01-14
Underlying this study is the hypothesized importance of insulin and glucose metabolism on bone. In our investigation of GIP and GIPR gene polymorphisms in relation to bone phenotypes in young and old women our findings depict a complex relationship between glucose metabolism genes and bone. In the c
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br Genetic manipulation variation of the ghrelin system
2022-01-13
Genetic manipulation/variation of the ghrelin system and alcohol-related outcomes Genetic manipulation of the ghrelin system (either the peptide or the receptor gene) via knockout rodent models has provided further insight into the role of this system in alcohol seeking and consummatory behaviors
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The intestinal epithelium is the
2022-01-13
The intestinal epithelium is the first line of defense against pathogens and noxious agents and exerts a range of physiological activities, including digestion and STF-118804 mg of nutrients. The intestinal wall consists of a series of finger shaped protrusions called villi and invaginations known
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In summary the SAR of a series of
2022-01-13
In summary, the SAR of a series of phenylpropanoic acid-free fatty Fluticasone propionate receptor agonists is described which resulted in the identification of potent FFA4 agonists. The superior pharmacokinetic properties of compound led to its selection as an in vivo tool compound which afforded
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We focus here on the
2022-01-13
We focus here on the historical discoveries that led to the development of the concept of ferroptosis. Ferroptosis is defined as an iron-dependent form of regulated cell death, which occurs through the lethal accumulation of lipid-based reactive oxygen species (ROS) when glutathione (GSH)-dependent
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br Materials and methods br Results br Discussion
2022-01-13
Materials and methods Results Discussion Type I ECa is associated with estrogen excess, obesity and hormone-receptor positivity. However, the function of ERα on ECa is considered complicated. The expression of ERα is reduced in grade III ECa clinical samples [13]. The high ERα expression is
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Among the isoforms of heme oxygenases
2022-01-13
Among the 3 isoforms of heme oxygenases (HO-1, HO-2, and HO-3), HO-1 expression is inducible, and it catalyzes the degradation of heme to biliverdin, carbon monoxide (CO) and free Fe. The Fe is then stored in ferritin, limiting its ability to participate as a catalyst through the Fenton reaction and
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br Acknowledgments This research was
2022-01-13
Acknowledgments This research was funded by generous grants from the Singapore National Medical Research Council (NMRC CBRG grant NMRC/CBRG12Nov114 (BD)). WJC is supported by NMRC Clinician Scientist Investigator award and partly supported by a Singapore Cancer Syndicate Grant, the National Resea
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HPgV coinfection has been associated with reduced liver dise
2022-01-13
HPgV coinfection has been associated with reduced liver disease in HPgV/HCV/HIV triply infected patients (Barbosa Ade et al., 2009, Berzsenyi et al., 2007, Berzsenyi et al., 2009, Berzsenyi et al., 2011). It is possible that HCV NS3 protease inhibitors could inhibit HPgV replication diminishing its
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