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Based on the previous report that FXR regulated
2022-04-12

Based on the previous report that FXR regulated PEPCK indirectly [20], we speculated that FXR may regulate gluconeogenesis by regulating some key transcription factors associated with gluconeogenesis. Finally, by using HS218 as a probe, we found that FXR binds to PGC-1α promoter and directly regulat
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In the present study VTE recurrence occurred in
2022-04-11

In the present study, VTE recurrence occurred in a non-cancer patient during edoxaban administration, representing recurrence rates of 1.7% in non-cancer patients and 0.8% in all patients. In a sub-analysis of cancer patients [27] and the main analysis [19] in the HOKUSAI-VTE trial, recurrent VTE oc
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The newly synthesized compounds were evaluated for their FAA
2022-04-11

The newly synthesized compounds were evaluated for their FAAH inhibitory activity in vitro. In addition, molecular modeling, selectivity and reversibility behavior of the new class of FAAH inhibitors are presented in this article. Results and discussion The potency of inhibition on the human rec
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To discriminate the peripheral and central involvement of FA
2022-04-11

To discriminate the peripheral and central involvement of FAAH in paracetamol action, we proposed a pharmacological strategy challenging the analgesic action of paracetamol observed in an inflammatory context with either a peripherally-restricted FAAH inhibitor (URB937, Clapper et al., 2010, Moreno
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br Funding The authors disclose the following support for
2022-04-11

Funding The authors disclose the following support for the research and/or authorship of this article: This work was supported by the Canadian Institutes for Health Research (CIHR). TM is the recipient of a BMS/CTN postdoctoral fellowship and PKQ was funded by a CAHR/CIHR doctoral scholarship. A
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Here we dissect X chromosome dosage compensation DC
2022-04-11

Here, we dissect X chromosome dosage compensation (DC) in C. elegans to determine the effect of chromatin modifications on higher-order chromosome structure during long-range gene regulation. DC is exemplary because it controls hundreds of genes simultaneously, it distinguishes X chromosomes from au
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br Mammalian chromosomal DNA binds to various proteins and
2022-04-11

Mammalian chromosomal DNA binds to various proteins and the DNA-protein complexes form DNA packaging units, called nucleosomes. Histones are the chief protein components of nucleosomes and perform pivotal functions in chromosomal gene regulation. Moreover, many types of chemical modifications of h
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Other N substituted carboxamide oxy pyridine derivatives a h
2022-04-11

Other N-substituted-6-carboxamide-3-oxy-pyridine derivatives 52a, 52h, 52i, and 53h were synthesized using an alternative route. The Pd-catalyzed Heck aminocarbonylation of 44 or 45 with (PPh3)2PdCl2 catalyst in the presence of Et3N under CO atmosphere successfully provided various N-substituted-6-c
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PDEs a group of metallophosphohydrolases hydrolyze the cycli
2022-04-11

PDEs, a group of metallophosphohydrolases, hydrolyze the 3′,5′-cyclic phosphate group on cyclic nucleotides to a 5′-monophosphate, thereby blocking cyclic AMP (cAMP) or cGMP signaling [8,9]. There are different types of PDE isozymes, with different substrate specificities. PDE5 (specific to cGMP) an
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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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br Rho protein networks in malignancy It
2022-04-11

Rho protein networks in malignancy It has long been recognized that Rho activity and expression are frequently elevated in tumors (Fritz et al., 1999, Orgaz et al., 2014). In this chapter we will introduce the most prominent Rho proteins, their regulators and effectors and provide an overview of
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Chronic exposure of cells to cytotoxic drugs can
2022-04-11

Chronic exposure of cells to cytotoxic drugs can result in the selection of multiple phenotypic and genetic changes. Thus, the use of MCF7/VP cells, which were selected for resistance to VP-16, was potentially problematic. However, a thorough characterization of MCF7/VP cells demonstrated that they
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br Introduction The replacement of a regular intake of
2022-04-11

Introduction The replacement of a regular intake of healthy oils and fibres for a diet based substantially on high fat- and high sugar-content foods has had profound consequences for public health. These changes in the way that the populations of high income, particularly Western countries, manag
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Peramivir br Introduction br Mitochondrial dysfunction
2022-04-11

Introduction Mitochondrial dysfunction and cancer Lactate and succinate as oncometabolites Intracellular actions of lactate and succinate as tumor promoters Cell-surface receptors for lactate and succinate and their role in cancer GPR109A as the receptor for butyrate and β-hydroxybu
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The opposite modulation observed for circulating LPI levels
2022-04-11

The opposite modulation observed for circulating LPI levels and WAT GPR55 Preladenant receptor by nutritional status suggests that increased levels of LPI may down-regulate the expression of its receptor in WAT, whereas in conditions of low serum LPI levels, the expression of GPR55 is stimulated. H
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