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HCV is a highly diverse virus
2022-04-11
HCV is a highly diverse virus with seven known genotypes (GT1–7) and multiple subtypes (Gower et al., 2014, Messina et al., 2015, Smith et al., 2014). Patients infected with HCV develop a heterogeneous population of viral species known as quasispecies due to low fidelity of the RNA-dependent RNA pol
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In summary P P macrocyclization proved to be an
2022-04-11
In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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br Methods br Results br Discussion Peptide
2022-04-11
Methods Results Discussion Peptide therapeutics represents a unique class of biopharmaceuticals that continues to evolve in drug discovery and development. We and others have been particularly interested in bioengineering innovative pGC-A and/or pGC-B peptide activators. This has been succe
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br Disclosure statement br Introduction Nitro phenylethane i
2022-04-11
Disclosure statement Introduction 1-Nitro-2-phenylethane is the first nitro compound isolated from plants [1]. It is a volatile compound found in the essential oil of various species, and its presence provides a pleasant odor that resembles the cinnamon scent [2]. The biogenesis of 1-nitro-2-p
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Interestingly studies from Sahai and colleagues in
2022-04-11
Interestingly, studies from Sahai and colleagues in cancer-associated fibroblasts have revealed that YAP is required for the acquirement of a stiff ECM in the tumor microenvironment (Calvo et al., 2013). Subsequently, this stiffening of the matrix can activate YAP, thus creating a feed-forward loop.
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It was reported that GPR is expressed on macrophages in
2022-04-11
It was reported that GPR120 is expressed on macrophages in adipose tissue (Oh et al., 2010). Whether GPR120-positive RK-33 synthesis in human and rat pancreas belongs to macrophages was studied. CD68 is a transmembrane glycoprotein that is highly expressed by human monocytes and tissue macrophages
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Due to the therapeutic potential of GlyT inhibitors numerous
2022-04-11
Due to the therapeutic potential of GlyT1 inhibitors, numerous drug screening campaigns have been started - and are still going on - which aimed at the identification of compounds with biological activity at or affinity for this drug target. For characterization of biological activity at GlyT1, tran
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It is an aspiring task to
2022-04-11
It is an aspiring task to apply the glutamate biosensor for in vivo measurements in 3787 tissue. Due to a relatively large size of the electrode used in this work, the biosensor fits only ex vivo applications. However, it is possible to apply platinum microelectrodes 50–100 μm in diameter for the b
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To further implicate the role of EAAT
2022-04-11
To further implicate the role of EAAT3 in morphine-induced place preference, the effects of morphine on EAAT3 UNC 0631 was determined. Interestingly, morphine increased EAAT3 protein expression in the plasma membrane of mPFC, nucleus accumbens and VTA but not in the hippocampus of wild-type mice at
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Recently accumulated evidence has revealed a
2022-04-09
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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According to the World Health Organization
2022-04-09
According to the World Health Organization, the average global intake of fat has increased by 20 g per person over the last half-century [21]. However, not all fats are the same and it is now well established that saturated and unsaturated fats, as well as trans fats, can act in opposing ways to inf
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First identified in as the
2022-04-09
First identified in 1982 as the second mammalian glutathione peroxidase [23], we and Stockwell's group demonstrated in 2014 that the selenoperoxidase GPX4 is the key upstream regulator of ferroptosis [12], [13]. The role of GPX4 as the main regulator in the ferroptotic process is based on its unique
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Autophagy plays a multifaceted role
2022-04-09
Autophagy plays a multifaceted role in regulating both the quality and quantity of protein (e.g., protein half-life and activity) and organelles (e.g., mitochondrial number and function), thus determining cell fate [15]. The induction of autophagy has been generally considered a programmed cell surv
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br Introduction Fructose bisphosphatase FBPase
2022-04-09
Introduction Fructose 1,6-bisphosphatase (FBPase; EC 3.1.3.11) catalyses the irreversible reaction of hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate and inorganic phosphate [1]. Genetic and kinetic studies so far have demonstrated that at least two distinct isoenzymes of FBPase e
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mitotic inhibitors The ability to metastasize is the definin
2022-04-09
The ability to metastasize is the defining character of a cancer and the leading cause for resultant mortality. It is hypothesized that a rare subset of cancer cells, often operationally referred to as “cancer stem cells” (CSCs), are responsible for sustaining cancer metastasis and recurrence [1]. T
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