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Although it has been observed
2022-02-12
Although it has been observed in numerous studies and by many investigators that intraplatelet cGMP elevation results in platelet inhibition, there are a few papers which proposed a platelet stimulatory role for cGMP when elevated in response to NO donors or PDE5 inhibitors in mouse and human platel
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Consistent with other studies on the
2022-02-12
Consistent with other studies on the metabolic effects of an OM3 enriched diet [26,104,105], irrespective of gender, the lowest glucose levels were seen in the Bob-Cat groups fed OM3 diet. Sexual dimorphism was observed in insulin levels. The highest average levels were in the HFD fed [Tg(CAT)±] mal
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br Conclusion The wild study reports seasonal
2022-02-12
Conclusion The wild study reports seasonal variations in reproductive physiology, behavior and Cholera Toxin plasticity at different age stages in wild-caught Mongolian gerbils. The gerbils in breeding seasons have more mature sexual development, higher exploratory behavior, higher novelty prefer
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Acarbose and voglibose the classic glucosidase inhibitors we
2022-02-12
Acarbose and voglibose, the classic α-glucosidase inhibitors, were clinically used to inhibit α-glucosidase activity for the treatment of type 2 diabetes. However, the intake of these drugs may cause some undesirable gastrointestinal side effects and weight gain (Xu et al., 2015). The synthetic drug
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Compounds were tested for GPR activity in a
2022-02-12
Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO ABC294640 mg transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activity r
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In conclusion a novel series of GPR
2022-02-12
In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen SB 415286 had a remarkable effect on the GPR40 agonistic activity.
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Sequences of HKI and HKII from humans were compared to
2022-02-11
Sequences of HKI and HKII from humans were compared to those of the Atlantic salmon to better understand the observation of HKI movement to the mitochondrial fraction in this study, as HKI in mammals is commonly assumed to be mostly passively regulated by product inhibition, with little evidence of
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We have shown previously that activation of
2022-02-11
We have shown previously that activation of the TGFβ/Smad signaling pathway in keratinocytes regulates RPC1063 cytoskeleton organization via non-genomic and genomic mechanisms and that RhoB gene is a target of Smad proteins [12,13]. Although the role of RhoB in early non-genomic TGFβ-induced cell r
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br Gastrointestinal peptides and intestinal health Gastroint
2022-02-11
Gastrointestinal peptides and intestinal health Gastrointestinal peptides are intimately involved in the regulation of feeding behaviors, energy metabolism and bodyweight 36, 37, 38, 39, 40, 41. GPR120 has been demonstrated to induce secretion of two such peptides: GLP-1 and cholecystokinin (CCK)
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As preclinical toxicity and efficacy both
2022-02-11
As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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It is becoming increasingly apparent that membrane lipids
2022-02-11
It is becoming increasingly apparent that membrane lipids play a critical role in modulating and regulating protein function. For example, embedding the homologous SLC1 transporter GltPh in a POPE bilayer allowed a third Na+ binding site to be identified from MD simulations [42], and the binding ene
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Peripheral injury or disease induced
2022-02-11
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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As early as glucagon was shown to increase energy
2022-02-11
As early as 1957, glucagon was shown to increase A-674563 expenditure in rodents in both pair-feeding studies and through directly increasing oxygen consumption [23], [24]. This has more recently been confirmed in man, through indirect calorimetry during glucagon infusions [25], [26], [27]. This co
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br Contributions br Acknowledgements This research was suppo
2022-02-11
Contributions Acknowledgements This research was supported by Natural Sciences and Engineering Research Council (NSERC) Discovery grant No. 341538 and Ontario Graduate Scholarships to HM and VS. Introduction Sexual size dimorphism describes size difference between male and female individua
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Ghrelin contains an n octanoylation at its
2022-02-11
Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat
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