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Tetrazole is one of the most commonly used
2022-06-14

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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Here we examined whether complete ablation
2022-06-14

Here, we examined whether complete ablation of GIP production could reduce weight gain in the absence of the adipocyte hormone leptin, a condition that results in extreme hyperphagia, obesity, hyperinsulinemia, and insulin resistance, in both mice [24] and humans [25]. We found that Lepob/ob mice be
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Both preclinical and clinical studies have identified a dist
2022-06-14

Both preclinical and clinical studies have identified a distributed set of CNS nuclei that participate in cognitive control of feeding behavior. Preclinical studies that utilize restricted access feeding schedules (RFS) indicate that rodents learn to anticipate delivery of scheduled meals as indicat
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Though regulation of ghrelin interaction with GHSR has not b
2022-06-14

Though regulation of ghrelin interaction with GHSR has not been described previously, a precedent for a similar regulatory mechanism exists in the form of the interaction between Agouti-Related Protein (AgRP) and melanocortin receptor subtypes MC3R and MC4R (Ollmann, 1997). AgRP is produced by hypot
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We are aware that the classical biochemical view is
2022-06-14

We are aware that the classical biochemical view is centered on the local concentrations of specific ion and molecules rather than on cell electric potentials. However, important downstream processes can be influenced by acting locally on these potentials because they regulate the conductance of the
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G quadruplex structures can be resolved
2022-06-14

G-quadruplex structures can be resolved by helicases. Consistently, many helicases are aberrantly expressed in cancer orexin [47]. In this study, we correlated HOXC10 expression with that of all helicases using a microarray dataset derived from 759 breast cancer patients [36] and discovered that CHD
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br Lung cancer cell lines The greatest expression of both
2022-06-14

Lung cancer cell lines The greatest expression of both human and rodent FFA4 transcript has been shown to be localized to the lung [61], yet the physiological role in this tissue has been understudied, as has its involvement in lung cancers. In 2015, a two-staged genome-wide association study of
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Folinic acid mg Compounds were tested for GPR activity in a
2022-06-14

Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO Folinic acid mg transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure acti
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br Importance of iron and lipoxygenase in ferroptosis What r
2022-06-14

Importance of iron and lipoxygenase in ferroptosis What remains to be somewhat controversial is the role of iron and lipoxygenases (LOX) in the death process, specifically in lipid peroxidation. So far, iron chelators have been repeatedly shown to halt ferroptosis (hence its name) induced by chem
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Accordingly and in animal models a high fat
2022-06-14

Accordingly and in animal models, a high-fat diet rich in CO (CO-HFD) impeded ventricular function and induced cardiac cell death and remodeling, at least, by down-regulating cell antioxidant defense systems and induction of oxidative stress [28], [29], [30], [31]. Interestingly, long chain fatty ac
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br Introduction A great many isoprenoids with varieties of s
2022-06-14

Introduction A great many isoprenoids with varieties of structural diversity, such as steroids, carotenoids, prenyl quinones, and natural rubber, occur in nature. All of these biosynthetic precursors are constructed by the action of prenyl chain elongating enzymes [1], [2], [3], [4]. These enzyme
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Andexanet alfa works as a decoy for the FXa
2022-06-14

Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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The cortical actin filaments are arranged in a network abuti
2022-06-14

The cortical Maraviroc synthesis filaments are arranged in a network abuting the plasma membrane with a thickness of ∼190nm in living cells, that displays highly dynamic behaviors 15, 16, 17. Technical challenges, however, have hampered investigation of the detailed function dynamic interactions be
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Fig summarizes the results for
2022-06-13

Fig. 1 summarizes the results for 500 μM concentration of the drugs. Action of histamine is presented for comparison. Both 1-methylhistamine and Nα-methylhistamine strongly potentiated ASIC1a responses. The concentration-dependence of action of Nα-methylhistamine was measured (Fig. 1B). Fitting by H
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Clonidine HCl Mammals adapt to prolonged periods of food sca
2022-06-13

Mammals adapt to prolonged periods of food scarcity by releasing FFAs from adipose tissue and transforming them into energy-rich ketone bodies that are used as fuel by brain, muscle, and other organs (Kersten, 2014, Grabacka et al., 2016). Ketogenesis occurs primarily in hepatocytes, but its rate i
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