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Despite efforts over the past
2022-03-03
Despite efforts over the past decade to shed light on the endosomal maturation process and its underlying Rab conversion, the context in which all the involved protein components interact needs to be further elucidated. After defining single components and modules of the machinery important for endo
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br Conclusion In this report we describe
2022-03-03
Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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Furthermore increased plasma levels of
2022-03-03
Furthermore, increased plasma levels of endoglin have been associated with diabetic complications (Valbuena-Diez et al., 2012). The involvement of soluble endoglin in a number of widespread pathologies demonstrates that endoglin is not only marker of endothelial integrity but also a causative factor
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In three independent groups identified
2022-03-03
In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niac
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Cichlasoma dimerus as most teleost fish species present
2022-03-03
Cichlasoma dimerus, as most teleost fish species, present neurons expressing GnRH3 (Pandolfi et al., 2005). As in most 493 species, the neurons expressing GnRH3 are mainly located in the NOR, although few neurons were detected in the olfactory bulb, ventral telencephalon and the POA (González-Martín
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On the basis of their relative
2022-03-03
On the basis of their relative Glu transport rates and anion currents, EAATs group into two functionally distinct classes, EAAT1–3 being efficient Glu transporters with small associated macroscopic anion currents and EAAT4–5 low-capacity transporters with predominant anion conductance [18]. The diff
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br Conclusion In summary a series of novel
2022-03-03
Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic ataluren motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing potent a
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br Acknowledgments This work was
2022-03-03
Acknowledgments This work was supported by a grant CIHR-NSFC China-Canada Joint Health Research from the National Science Foundation of China (Grant Number 81061120525) and the Canadian Institutes for Health Research (Grant number CCI-109605). The authors thank two anonymous reviewers for helpful
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Introduction Initially postulated to represent the main sour
2022-03-02
Introduction Initially postulated to represent the main source of ATP production in eukaryotic cells, mitochondria are recently recognized to perform manifold essential functions beyond energy production, impacting most areas of cell biology and medicine [1]. Mitochondrial metabolism is both the ba
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Moreover intestinal chronic inflammation is
2022-03-02
Moreover, intestinal chronic inflammation is a promoting factor in the development of CRC in patients affected by inflammatory bowel disease (IBD), such as Crohn's disease and ulcerative colitis. We have previously shown that pharmacological FXR activation via its ligand obeticolic Licofelone count
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Clinical data showed TAK was
2022-03-02
Clinical data showed TAK-875 was rapidly absorbed with a half-life of 28-30h and clearance primarily through glucouronidation in the liver with minimal urinary clearance [30]. TAK-875 made the glycosylated hemoglobin (HbA1c) levels fall significantly from baseline after 24-week administration in onc
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hcv protease inhibitors br Materials and methods br Results
2022-03-02
Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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Literature review suggests a strong presence of central hist
2022-03-02
Literature review suggests a strong presence of central histaminergic transmission in the AR-M 1896 areas targeted by caffeine to induce its behavioral actions. Interestingly, it is reported that caffeine administration increases the histamine neuronal activation and release of histamine in the brai
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br Histamine and glycaemia Histamine is involved in
2022-03-02
Histamine and glycaemia Histamine is involved in a wide variety of pathophysiological events mostly related to the inflammatory response through four receptors, namely H1-4Rs. The first studies of Mirin and diabetes date back to the 1950s. Since that time the involvement of histamine in diabetes
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br Materials and methods br Results br Discussion CRC
2022-03-02
Materials and methods Results Discussion CRC and PC occupy a good share in cancer-related deaths worldwide. CRC is a common gastrointestinal malignancy with a growing incidence whereas PC is one of the most dreadful malignancies with extremely poor survival rates. Though over the past decad
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