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br Factor Xa an enzyme
2022-06-09

Factor Xa, an enzyme in the coagulation cascade, has recently been identified as having a role in inflammation, generating interest in factor Xa inhibitors as anti-inflammatory agents beyond their established use as anticoagulants [, , , ]. We report sustained clinical and electrophysiologic impro
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It is known that microglial function
2022-06-09

It is known that microglial function and morphology are closely related [20], but no studies have addressed whether neuroinflammation induced by alcohol might modify microglial Losmapimod (i.e. morphology, neuroimmunochemical phenotype) through an eCB-dependent mechanism. Since this alcohol-induced
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On the other hand G a
2022-06-09

On the other hand, G9a/GLP could also alter neuronal function without directly altering the transcription level of particular plasticity-related protein: the consolidation of early-LTP to late-LTP, as well as the reversal of mGluR-LTD by G9a/GLP inhibition required PKMζ translation and its downstrea
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Thus both in Drosophila and mammals
2022-06-08

Thus, both in Drosophila and mammals, the Hippo pathway responds to cell–cell junctions via an apical NF2/Mer-containing complex. Indeed, Hippo signalling and NF2 are required for contact inhibition of growth in cell culture, which is thought to reflect an in vivo function as a sensor of tissue crow
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GSTP is a class Glutathione
2022-06-08

GSTP1 is a π-class Glutathione S-transferase (GST-π) enzyme involved in tumor suppression by protecting sglt inhibitors against genomic damage mediated by various oxidants. Although the loss of GSTP1 function by hypermethylation has been reported as a common epigenetic alteration in prostate carcino
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br Materials and methods br Results Our data indicated
2022-06-08

Materials and methods Results Our data indicated that 1,8-cineol leads to a noticeable but not significant (p = 0.07) 45% decreased phosphorylation of GSK-3α/β at Ser-9/21. Phosphorylation of GSK-3α/β at Tyr-279/216 was not affected (Fig. 1A/B). To ensure, that the decreased phosphorylation of
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br Results br Discussion We have
2022-06-08

Results Discussion We have reported the crystal structures of VcmN, the high-resolution structures of this MATE transporter from a pathogenic bacterium. The structures display distinct conformations of TM1, as a consequence of their unique hydrogen-bonding networks. We interpret this result to
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PBI is an agonist of
2022-06-08

PBI-4050 is an agonist of GPR40 and acts as an antagonist or inverse agonist of GPR84. It cannot be excluded that other targets besides GPR40 and GPR84 could be implicated in the mechanism of action of PBI-4050 and could be explored in future studies. However, the present study, and in particular th
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An increased sympathetic tone and
2022-06-08

An increased sympathetic tone and the hormone glucagon are the main glucose mobilizing factors [28], [29]. Single-cell transcriptome analysis of human islet cells suggests the expression of Ffar1 not only in β-cells but also in α-cells [30]. Moreover, analysis of rat α-cells indicates that FFAR1 exp
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Newt GHS R a proteins
2022-06-08

Newt GHS-R1a proteins expressed in a mammalian cell were able to bind homologous newt ghrelin, heterologous rat and bullfrog ghrelin, and a peptidyl GHS-R1a agonist, GHSRP-6, with inducing intracellular Ca signaling. This indicates that the identified cDNA encodes the ghrelin receptor from a view of
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MMV s distinct mode of inhibition
2022-06-07

MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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There are several basic science studies that aim to
2022-06-07

There are several basic science studies that aim to investigate potential mechanisms behind the reduced incidence of MI in factor Xa inhibitor treated patients. Perzborn et al. reported that in-vitro addition of rivaroxaban reduced tissue-factor induced platelet aggregation (Perzborn, Heitmeier, & L
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The site of paracetamol action remains controversial
2022-06-07

The site of paracetamol action remains controversial. Some publications are in favor of a central action (Barrière et al., 2013, Dogrul et al., 2012, Mallet et al., 2010, Pickering et al., 2006), while others report a peripheral action (Dani et al., 2007, Ferreira et al., 1978). FAAH is a ubiquitous
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br Experimental br Results and discussion One
2022-06-07

Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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Lastly certain populations of immune cells
2022-06-07

Lastly, certain populations of immune cells may be Hh responsive. Although PC have not been demonstrated in healthy liver-resident macrophages or lymphocytes, macrophages in injured livers have been shown to produce Hh ligands[58], [100], [101] and treating liver-derived macrophages with neutralisin
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