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On the basis of their relative
2021-09-09

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
2021-09-09

Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic Boc-Phe-Osu 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 poten
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In prostate cancer PCa glucose metabolism
2021-09-09

In prostate cancer (PCa), glucose metabolism plays a major role in progression [14]. Androgens can activate the metabolic regulator AMP-activated kinase (AMPK), promoting oxidative phosphorylation (OXPHOS) [15]. Besides, androgens increase GLUT1 [16], which overproduction has been described in the m
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Acarbose and voglibose the classic
2021-09-09

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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br Materials and methods br Results
2021-09-09

Materials and methods Results and discussion Conclusions Acknowledgments The authors are grateful to Dr. N. Prevete for providing the human AGS shCTR and AGS shFPR2 cells. This work was supported by POR Campania FSE 2007-2013 Project CREME and Ministry of Health, Italy, RF-2011-02349269.
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niclosamide A general synthesis of the tetrazole is shown in
2021-09-09

A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic niclosamide followed by reduction of the
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Our observation of LPS induced increase
2021-09-09

Our observation of LPS-induced increase in the sensitivity of cultured endothelium-intact coronary Quinupristin-Dalfopristin Complex mesylate towards stimulation with selective ETB receptor agonist (S6c) could be explained by activation of TLRs receptors located on the endothelium of rat coronary a
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Accumulating evidence suggests that the NGF family of
2021-09-09

Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, erk inhibitors derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37]. BDNF knock
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In an effort to more fully explore the structure
2021-09-09

In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold
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HOBt mg br Materials and methods br Results
2021-09-09

Materials and methods Results Discussion Several histamine H3 receptor antagonists have progressed into clinical development for indications including Alzheimer's disease, schizophrenia, pain and narcolepsy. Each of the compounds studied herein has been extensively characterized in its own
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br Histamine and glycaemia Histamine is involved in
2021-09-09

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 3965 synthesis and diabetes date back to the 1950s. Since that time the involvement of histamine in
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Methimazole sale Recently the spectrin cytoskeleton a
2021-09-09

Recently, the spectrin cytoskeleton, a deformable actin-associated network, has been identified as a modulator of Yki function, potentially acting both apically and basally in different cell types [75•, 76•, 77•]. Several mechanisms have been proposed, including regulation via Crb/Ex tethering [], t
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RS testing has been extensively validated in patients with
2021-09-09

RS testing has been extensively validated in patients with early stage, ER+, HER2− patients. TAILORx, a randomized controlled trial to evaluate the role of adjuvant chemotherapy by RS, found no recurrence or survival benefit to the addition of chemotherapy to endocrine therapy in patients with inter
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br Acknowledgements br Introduction Type diabetes is
2021-09-08

Acknowledgements Introduction Type 2 diabetes is a progressive metabolic disorder which is characterised by chronic hyperglycaemia due to relative insulin deficiency, insulin resistance and increased hepatic glucose production [1]. The metabolism of glucose by glycolysis increases the ATP:ADP
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Moreover there is a third possible GnRH
2021-09-08

Moreover, there is a third possible GnRH agonist target – the endometrium. The human endometrium has been shown to express high levels of both GnRH and GnRH receptors (Maggi et al., 2016), and GnRH agonists affect the function of the urokinase-type plasminogen activator/plasminogen activator inhibit
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