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2449 In addition researchers studying GPR agonists favor
2022-06-02

In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it 2449 is unclear why Sanofi-Aventis chose to terminate collaboration with Metabolex (now
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GnRH receptor GnRH R levels are elevated in decidualized
2022-06-02

GnRH receptor (GnRH-R) levels are elevated in decidualized stromal cells, suggesting a function for the GnRH–GnRH-R pathway in the early implantation events. Both GnRH and GnRH-R have been shown to be present in preimplantation embryos and the fallopian tubes at both mRNA and protein levels (). Two
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The synthesis of is shown in The
2022-06-02

The synthesis of is shown in . The ---Boc--diaminopropanoic acid--butyl ester () fragment was synthesized in four steps from Boc--asparagine (). The key step in this synthesis was a Hofmann rearrangement of the terminal carboxamide, which was performed according to the elegant protocol of Zhang tha
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Previous studies have suggested that GPR protects from bone
2022-06-01

Previous studies have suggested that GPR40 protects from bone loss via inhibition of osteoclasts. Wittrant et al. used GPR40 knock-out mice and primary osteoclasts to investigate the role of GPR40 on bone remodelling. Their results in primary osteoclast cultures and the RAW264.7 cell line showed tha
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In mammals the primary cilium is considered a hub for
2022-06-01

In mammals, the primary cilium is considered a hub for signal transduction. The cilium has previous been associated with transduction of several pathways including Wnt (Corbit et al., 2008, McDermott et al., 2010, Tran et al., 2014), PDGF (Clement et al., 2013, Schneider et al., 2010, Schneider et a
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br Introduction The growth hormone
2022-06-01

Introduction The growth hormone secretagogue receptor (GHSR) gene, which was first isolated from rats and humans (Kojima et al., 1999), comprises two exons and one intron in mammals and chicken. The pig GHSR is located on chromosome 13 (range 110,981,465–111,006,149 on Reference Sscrofa11.1). Alt
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Acknowledgements br Introduction Alzheimer s
2022-06-01

Acknowledgements Introduction Alzheimer's disease (AD) is a devastating neurodegenerative disorder and the leading cause of dementia. There is currently no treatment available to slow or halt disease progression. The underlying mechanisms of AD on the cell and molecular levels are still not comp
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Notch signaling maintains the balance between neural stem ce
2022-06-01

Notch signaling maintains the balance between neural stem cells and neural progenitors (Aguirre et al., 2010, Basak and Taylor, 2007, Mizutani et al., 2007). Conditional knock out of Notch causes depletion in the progenitor pool, showing that Notch is required for the maintenance of neural stem cell
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To date types of glucose
2022-06-01

To date, 14 types of glucose transport protein have been discovered, each having its own specific functions with different distributions [33]. Among these, GLUT4 is particularly important for maintaining glucose metabolism homeostasis and insulin sensitivity, since it is involved in glucose transpor
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biperiden Methoxyflavone and methoxyflavanone Fig both act a
2022-06-01

6-Methoxyflavone and 6-methoxyflavanone (Fig. 2) both act as flumazenil-insensitive positive allosteric modulators of GABA responses at human recombinant α1β2γ2L and α2β2γ2L GABAA receptors. However, unlike 6-methoxyflavone, 6-methoxyflavanone was relatively inactive at α1β2 GABAA receptors. Both fl
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receptor tyrosine kinase Recently Bristol Myers Squibb and M
2022-06-01

Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic receptor tyrosine kinase derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole
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The central event eliciting insulin secretion is the product
2022-06-01

The central event eliciting insulin secretion is the production of ATP which leads to the inhibition of ATP-sensitive inwardly-rectifying K+ATP channels, a consecutive depolarization of the plasma membrane with opening of voltage-dependent Ca2+ channels and Ca2+ influx into the beta-cell. However, i
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br Materials and methods All studies were
2022-06-01

Materials and methods All studies were performed in 230–250g timed-pregnant Sprague Dawley rats (Harlan, Indianapolis, Indiana). Animals were housed in a temperature controlled room with a 12:12 light:dark cycle. All experimental procedures in this study were in accordance with the National Insti
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More specific quantitative assays for DiXaIs are based on th
2022-06-01

More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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DOI hydrochloride br What are the local
2022-06-01

What are the local exocytotic protein targets of PKC? A direct method for PKC to potentiate insulin release would be to phosphorylate and activate components of the exocytotic machinery. Bulk measurements show that potentiation occurs by enhancement of the calcium sensitivity of exocytosis [56],
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