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NPxY was recognized as the first short signal
2022-01-30

NPxY was recognized as the first short signal sequence motif in the cytoplasmic domain of membrane receptors and proteins with critical roles in internalization and trafficking of receptor molecules [130]. Including LDL receptor, beta-1 integrin, megalin, beta-amyloid precursor protein, EGF receptor
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One of the possible disadvantages of this
2022-01-30

One of the possible disadvantages of this methodology is a possible cytotoxic effect resulting from either adenoviral vector injection or to Cre recombinase expression. Adenovirus has previously been used to efficiently mediate transgene expression in mouse ac 723 (Thomas et al., 2000, Xia et al., 2
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Discrepancies in the reported results and conclusions from d
2022-01-30

Discrepancies in the reported results and conclusions from different groups regarding studies in ghrelin−/− and ghsr−/− mice are likely explained by the mixed background of the mutant mice used in the different studies [35]; although in the case of mice exposed to HFD, exposure to a HFD immediately
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We and others have previously reported that
2022-01-30

We and others have previously reported that neurons generated from iPSCs with genetic forms of AD recapitulate aspects of the disease, including increased Aβ peptide production in trisomy 21 and APP duplication neurons (Moore et al., 2015, Israel et al., 2012) and increased production of longer form
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In our study the changes
2022-01-30

In our study, the changes in the α4 and δ subunit expression were accompanied by a significant increase in γ2 subunit expression in almost all analysed hippocampal structures in the fully kindled animals. In contrast, an acute injection of PTZ at a convulsive dose (55mg/kg) evoked a potent decrease
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br Acknowledgements We apologize to our
2022-01-30

Acknowledgements We apologize to our distinguished colleagues whose work has not been cited owing to space limitations. This work was funded by the Italian Association for Cancer Research (AIRC, Milan, Italy, IG 14732 to A.M.); Italian Ministry of University and Education (Finanziamenti per la Ri
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br Introduction Hepatocyte injury initiates and
2022-01-30

Introduction Hepatocyte injury initiates and facilitates inflammation in the course of liver disease progression. Thus, understanding the regulatory basis for sensing and responding to damage-associated inflammatory processes in the liver’s parenchymal cells is a primary issue in liver pathophysi
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Thrilled by these promising results our quest for discoverin
2022-01-30

Thrilled by these promising results, our quest for discovering new PPAR-γ/FFAR1 co-agonists was directed towards exploring the other two new scaffolds. So, in this proposed manuscript, we will describe our efforts regarding the synthesis, biological evaluation and molecular docking studies of the be
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br Significance Metabolites present in the
2022-01-30

Significance Metabolites present in the extracellular environment can potently modulate cellular phenotypes and potentially serve as therapeutics for various diseases. Ferroptosis is a non-apoptotic cell death process characterized by the generation of toxic lipid reactive oxygen species (ROS). I
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In order to understand the determinants of high
2022-01-30

In order to understand the determinants of high affinity of with amide side chain, an X-ray crystal structure of human liver FBPase in complex with was determined (). The position of phosphonate group and tricyclic scaffold of is similar to those of with no side chain, which suggests the formation o
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It is interesting that SEC
2022-01-29

It is interesting that SEC significantly inhibited cell migration and EMT in PC3 cells expressing a low RKIP level and HEK293T RKIP−/− cells, while had no effect on HEK293T RKIP+/+ cells. These observations can be interpreted that the RKIP-ANXA7 association may block SEC-induced ANXA7 GTPase activat
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br Acknowledgements br Introduction The glutathione S
2022-01-29

Acknowledgements Introduction The glutathione S-transferase (GST, EC 2.5.1.18) family of multifunctional enzymes plays a particularly important role in cellular detoxification [1]. Over-expression of the GSTP1 isoform characterizes many human tumor cell lines derived from stomach, brain and co
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Having identified initial leads and
2022-01-29

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic PHA-665752 receptor derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, met
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With this goal in mind
2022-01-29

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in acti
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Previous studies have suggested that GPR protects from
2022-01-29

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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