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Since primitive societies plants herbs and seeds rich in
2023-01-10

Since primitive societies, plants, herbs and seeds, rich in phytochemicals, were used due to their benefits in human health. These molecules were shown to present a diverse array of action mechanisms, including antioxidant activity, enzyme stimulation, hormones mimicking and by interfering with DNA
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br Implementation of sacubitril valsartan into
2023-01-10

Implementation of sacubitril/valsartan into clinical practice Following on from the results of PARADIGM-HF, sacubitril/valsartan was given regulatory approval for use in patients who conform to the main inclusion criteria of the trial; NYHA functional class II–IV, reduced left ventricular ejectio
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Through an extensive SAR optimization campaign with
2023-01-09

Through an extensive SAR optimization campaign with the 4-((2-hydroxy-3-methoxybenzyl)amino)-benzenesulfonamide-based scaffold researchers have developed ML355 ((N-benzo[d]thiazol-2-yl)-4((2-hydroxy-3 methoxybenzyl)amino)benzenesulfonamide) [5]. ML355 is a nonreductive, noncompetitive, reversible 12
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Unexpectedly under pathological pain conditions inhibition o
2023-01-09

Unexpectedly, under pathological pain conditions, inhibition of spinal glutamate transporter activity can produce antinociceptive effects. For example, intrathecal injection of the transportable inhibitor trans-pyrrolidine-2,4-dicarboxylic BI-9564 australia (t-PDC) or antisense oligonucleotides red
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br A Rs which were
2023-01-09

A3Rs, which were cloned and then pharmacologically identified in the early 1990s, are expressed in multiple organs and peripheral tissues including ptio involved in inflammatory responses (Gessi et al., 2008, Borea et al., 2014). While low levels are expressed in the CNS, A3R agonists produce fun
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br ATX LPA pathway in animal models
2023-01-09

ATX–LPA pathway in animal models of rheumatoid arthritis Several animal models have been used to characterize the mechanisms involved in the pathogenesis of arthritis and to test new therapeutic strategies. The collagen-induced arthritis (CIA) model (Courtenay et al., 1980, Luross and Williams, 2
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Further analysis sought to understand the mechanism
2023-01-09

Further analysis sought to understand the mechanism associated with the autotaxin-mediated increase of miR-489-3p in circulation. Based upon sequence complementarity, DIANA TarBase predicted miR-489-3p targets MAPK2K1, or MEK1, an oncogene widely dysregulated in cancer (Fig. 4A). To test this relati
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br Introduction Lung cancer is the leading cause
2023-01-09

Introduction Lung cancer is the leading cause of cancer death worldwide and is one of the most refractory of solid tumors along with pancreatic cancer. Since 1975 there have been notable improvements in the 5-year survival rate of patients with lung cancer [1]. This improvement in survival is tho
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Previous studies have demonstrated ATR inhibition is
2023-01-09

Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia gamma secretase inhibitor to enhance chemotherapy sensitivity [[16], [17], [18],[20]
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Why do glutamate and glycine
2023-01-09

Why do glutamate and glycine bind to the inhibitor of catalase in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the
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The approach of enzymatically converting an
2023-01-09

The approach of enzymatically converting an analyte and detecting it by the resulting small pH changes near the reduced graphene oxide (rGO) surface has successfully been pursued in case of urea (Piccinini et al., 2017). Furthermore, this work reported that electrostatic layer-by-layer (LbL) assembl
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A next series of experiments explored
2023-01-09

A next series of experiments explored whether cardiac Ampkα1 nucleoside analogs is modified in response to pressure overload imposed by TAC. As a result, 2weeks of TAC treatment significantly increased Ampkα1 protein abundance in cardiac tissue from Ampkα1+/+ mice as compared to sham treated mice (
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Another class of AMPK regulator
2023-01-09

Another class of AMPK regulator is peptidyl-prolyl cis/trans isomerase (PPIase) NIMA-interacting 1 (Pin1), which binds to a number of proteins and regulates oncogenesis and metabolic diseases (Khanal et al., 2013; Zhou and Lu, 2016). Pin1 has been shown to bind to and inhibit AMPK; therefore, at lea
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Despite hydrolysis with commercial enzymes like trypsin peps
2023-01-05

Despite hydrolysis with commercial enzymes like trypsin, pepsin, Alcalase, Flavourzyme and Thermolysin have been used to digest parent proteins and generate peptides, microbial fermentation by proteolytic species has also proved to be a successful strategy (Fakhfakh et al., 2013, Jemil et al., 2016,
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The interaction of ATR ATRIP with
2023-01-05

The interaction of ATR-ATRIP with RPA-coated ssDNA is sufficient for ATR-ATRIP recruitment to DNA lesions, but it is not sufficient to fully activate ATR. In response to DNA damage, the heterotrimeric ring-shaped complex 9-1-1 (RAD9-RAD1-HUS1 in humans; Ddc1-Rad17-Mec3 in S. cerevisiae) is loaded at
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