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Recently accumulated evidence has revealed
2022-06-22
Recently, accumulated evidence has revealed a close link of FXR to gluconeogenesis. For example, activation of FXR by its agonist GW4064 improved hyperglycemia in db/db mice by repressing gluconeogenesis [15], and FXR agonist CDCA decreased transactivation activity of key gluconeogenic genes by indu
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Type II diabetes is characterized by an inability to
2022-06-22
Type II diabetes is characterized by an inability to maintain glucose homeostasis due to insulin desensitization and/or insufficient insulin secretion. GPR40, also known as free fatty Benzoylhypaconitine receptor 1 (FFAR1), is a member of the G-protein-coupled lipid-activated family of receptors an
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Arsenic is generally found in the
2022-06-22
Arsenic is generally found in the form of iAs in arsenic plants. Arsenic is primarily metabolized in the liver through methylation processes. Human metabolism of arsenic results in the formation of the methylarsenic metabolites, MMA and DMA, which are more water soluble (Khaleghian et al., 2014; Wei
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The synthesis of substituted pyrimidinone carboxamides is ou
2022-06-22
The synthesis of 2-substituted pyrimidinone carboxamides – is outlined in , . Treatment of readily accessible nitriles with N-methylhydroxylamine hydrochloride in the presence of GSK1059615 provided the adducts , which were subsequently reacted with diethyl acetylenedicarboxylate to afford insepar
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Migration chemotaxis and trafficking of leukocytes including
2022-06-22
Migration, chemotaxis and trafficking of leukocytes, including eosinophils from the peripheral blood into the site of inflammation requires their adhesion to endothelial Phenytoin sodium (Ley et al., 2007). Despite ongoing research, the histamine effect on eosinophils adhesion to endothelium cells h
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PF-8380 br Conclusion In conclusion HER CTCs can be
2022-06-22
Conclusion In conclusion, HER2+ CTCs can be detected using the LiquidBiopsy system. Among the patients with histologically HER2+ breast cancer, 41.9% had ≥ 1 HER2+ CTC/4 mL of blood. The cell lines experiments showed high sensitivity (100%) and specificity (99.9%) using a HER2/CD45 fluorescence r
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Telbivudine br Conclusion and perspectives Guanylyl cyclases
2022-06-22
Conclusion and perspectives Guanylyl cyclases are ubiquitous enzymes that regulate critical functions in bacteria to humans. In mammals there are seven mGCs and activators of all members have now been identified. Mutations in the genes that encode mGCs or pathologic activation of these enzymes or
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Using embelin and its analogs
2022-06-22
Using embelin and its analogs as surrogate GPR84 agonists we discovered that GPR84 couples to G12 and G13 signaling pathways in addition to Gi, linking receptor function to Rho/Rac signaling and modulation of the cytoskeleton. In primary human macrophages, GPR84 activation leads to Gβγ signaling, Er
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The amyloid precursor protein APP
2022-06-21
The amyloid precursor protein (APP) is a membrane protein thought to be involved in plasticity, synapse formation and repair, and export of metal ions [68]. The APP present in the brain can be cleaved by three different secretases [73], [74]. Cleavage of APP first by alpha secretase and then gamma-s
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In vitro studies have shown that some antidepressant drugs b
2022-06-21
In vitro studies have shown that some antidepressant drugs bind to NMDA receptors and inhibit the binding of NMDA receptor ligands [18]. Similarly, several research teams have reported that tricyclic antidepressants can modulate the release and/or uptake of glutamate [19]. In this study, we found th
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Although the ramifications of non additive
2022-06-21
Although the ramifications of non-additive SAR are context-dependent, the knowledge that perturbations in one region of a chemical series are not synergistic with perturbations in another region of the same chemical series is clearly pertinent to any medicinal chemistry effort. In our experience, no
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br Ghrelin interactions with the opioid system The endogenou
2022-06-21
Ghrelin interactions with the opioid system The endogenous opioid system is an important regulator of appetite and metabolism (Bodnar, 2017, Nogueiras et al., 2012). In fact, several pharmacological studies have demonstrated that agonists of the three opioid receptors (mu, kappa, and delta) incre
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br The small conductance Ca activated K SKCa SK
2022-06-21
The small conductance Ca-activated K+ (SKCa; SK, SKCa, KCa2) channels are recognized as a subfamily of KCa channels (Bond, Maylie, & Adelman, 1999). The SKCa channel is encoded by three distinct genes, KCNN1, KCNN2, and KCNN3 with different sensitivities toward apamin. Different with BKCa channels
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Yes mutations have been linked to two main types
2022-06-21
Yes, mutations have been linked to two main types of disorder in humans. Several autosomal dominant mutations, some of which have been characterized and lead to increased PIEZO1 signaling, are associated with dehydrated hereditary stomatocytosis (DHS). DHS is characterized by osmotically-driven d
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Introduction br Alzheimer pathology A and Tau Amyloid protei
2022-06-21
Introduction Alzheimer pathology: Aβ and Tau Amyloid β protein (Aβ) plays an important role in AD pathogenesis. At the molecular level, senile amyloid plaques and neurofibrillary tangles (NFT) are two neuropathological hallmarks of AD [1]. Mutations in genes encoding amyloid precursor protein (A
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