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One of the most common dietary approaches against
2022-04-20

One of the most common dietary approaches against obesity-associated diseases is the increase in the consumption of ω3 polyunsaturated fatty acids [18], [19]. Since seminal paper by Bang and Dyeberg in which the low prevalence of coronary heart disease among the Inuit was associated with the high ma
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br Conclusion br Acknowledgements This work was supported
2022-04-20

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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Cy5 maleimide (non-sulfonated) Herein we report the discover
2022-04-20

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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To further investigate if GPR was the
2022-04-20

To further investigate if GPR40 was the functional target of these phenylpropiolic Azidobutyric acid NHS ester analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux
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Accordingly it is tempting to
2022-04-20

Accordingly, it is tempting to speculate that the maintenance of a stimulus representation in the A2 state for a short period of time after the presentation of a specific stimulus (i.e. self-generated priming) may rely upon GluR-A-dependent synaptic plasticity. If this were the case, GluR-A semagace
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br Introduction Glucagon is a peptide hormone
2022-04-19

Introduction Glucagon is a peptide hormone that acts to increase blood glucose levels. The secretion of glucagon from the alpha BPTES of the islets of Langerhans in the pancreas is increased during fasting and prevents hypoglycemia. Glucagon increases glycogenolysis and gluconeogenesis and there
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GHRL effect on appetite is
2022-04-19

GHRL effect on appetite is influenced by its dose and route of administration, where central or peripheral administration of GHRL at low doses increases feed intake, via acting on orexigenic hypothalamic neurons, and decreases appetite at high doses in chickens (Jonaidi et al., 2012), quails (Shoush
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In a previous paper we demonstrated immunohistochemically th
2022-04-19

In a previous paper, we demonstrated immunohistochemically the USA of GHSR-1a in acrosomes and peripheral region of spermatid heads as well as in acrosomes of the spermatids undergoing spermiation [19]. The present study was undertaken to demonstrate the GHSR-1a expression in rat epididymal spermato
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The focused set of cyclopentapyrazoles produced six compound
2022-04-19

The focused set of cyclopentapyrazoles produced six compounds with sufficient activity to warrant the evaluation of kinetic solubility. Despite the improved activity of the series, these compounds remain stalwartly insoluble (), indicating the need for additional chemical modifications which address
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Introduction galactosidase d galactoside galactohydrolase
2022-04-19

Introduction β-galactosidase (β-d-galactoside galactohydrolase or lactase; EC 3.2.1.23) is an important type of glycoside hydrolase that can catalyze the conversion of lactose to uric acid and galactose. Furthermore, it can also catalyze transglycosylation reactions, which are usually used for the
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During the course of our optimization of
2022-04-19

During the course of our optimization of the diarylsulfonamide chemotype as FFA4 agonists, we identified xanthene as a potent and selective antagonist of FFA4 (). Xanthene was able to block the agonist induced intracellular Ca response elicited by both linoleic Ginkgolic Acid C15:1 and compound in c
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In early a collaborative effort between the group that
2022-04-19

In early 2017, a collaborative effort between the group that pioneered the above described evidence of platinum-induced PUFA chemotherapy resistance and a group that has contributed to much of the known molecular pharmacology of FFA4, revealed that the molecular target of 16:4(n-3), which affords ch
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ATN Ac PHSCN NH is a
2022-04-19

ATN-161 (Ac-PHSCN-NH2) is a small peptide antagonist of integrin α5β1, a recently developed anticancer drug that interacts with the N-terminus of the β1 region of integrin α5β1 to lock integrin α5β1 in its non-activated conformation (Wang et al., 2016). The drug has been tested in Phase 2 clinical t
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Another strategy adopted to enhance the
2022-04-19

Another strategy adopted to enhance the action of endocannabinoids is indirectly through blocking their metabolism. Indeed, amplifying the action of anandamide and 2-AG by inhibiting their enzymatic degradation has emerged to develop the endocannabinoid system for medicinal purposes. It is interesti
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The site of paracetamol action remains controversial Some pu
2022-04-19

The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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