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Calcipotriol Hexokinases HXKs are major regulatory enzymes i
2021-12-29

Hexokinases (HXKs) are major regulatory enzymes in sugar metabolism and in sugar sensing in plants (Claeyssen and Rivoal, 2007, Granot et al., 2013, Sheen, 2014, Aguilera-Alvarado and Sánchez-Nieto, 2017). HXK can phosphorylate both glucose and fructose to respective hexose-6-phosphates as a first s
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br Heme and the HO system
2021-12-29

Heme and the HO system Heme, a complex of iron and protoporphyrin IX, has versatile functions, which are critical for the survival of all aerobic organisms including mammalians and bacteria [9]. The central iron in heme facilitates six ligand binding sites [10], four of which are occupied by nitr
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Several studies have found that GPR possesses a distinct pha
2021-12-29

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected Triclosan expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rim
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ATP as a transmitter can be released from injured
2021-12-29

ATP as a transmitter can be released from injured 1,2-Dimyristoyl-sn-glycerol and sensory nerve endings (Sperlágh et al., 1995, Sperlágh et al., 1997, Sperlágh et al., 1998, Burnstock, 2013, Burnstock, 2014). ATP can activate the P2X3 receptor in the DRG neurons (Gao et al., 2011a; Xu et al., 2012)
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br Inclusion exclusion criteria br Quality assessment All st
2021-12-29

Inclusion/exclusion criteria Quality assessment All studies included in the qualitative synthesis were evaluated using the Quality Assessment Tool for Quantitative Studies (QATQS), which allows to determine their methodological quality. QATQS assesses 8 sections: selection bias, study design,
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br Materials and methods Rat forebrains were obtained from S
2021-12-29

Materials and methods Rat forebrains were obtained from Sprague–Dawley rats at 2, 7, 14, 21, and 30–35 postnatal days and were homogenized in 1:5 volumes (w/v) of 0.32 M sucrose containing 1 mM EGTA, 1 mM EDTA, 1 μg/ml TPCK, 50 μM leupeptin, and 3 μM antipain with 10 strokes in a glass-teflon hom
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Type diabetes mellitus is characterised by two major feature
2021-12-29

Type 2 diabetes mellitus is characterised by two major features: peripheral insulin resistance and impaired insulin secretion from pancreatic beta GW0742 synthesis [1]. The condition occurs when the pancreatic beta cells are unable to compensate for increased insulin demand due to insulin resistanc
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Animal studies have shown that
2021-12-29

Animal studies have shown that various antidepressant treatment are capable of upregulating GR protein and mRNA in key Piperine regions including the hippocampus and decreasing basal and/or stress-induced glucocorticoid secretion [37]. Changes in the level or function of GR regulate the negative fe
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Our initial lead optimization started with the
2021-12-28

Our initial lead optimization started with the modification of the indole head group as summarized in . Extensive exploration indicated that there was limited tolerance of structural change in this region of the molecule. All of the modifications to the indole moiety, including N-substitution (), li
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Different from stable transfection transient expression was
2021-12-28

Different from stable transfection, transient expression was also found to yield γ-secretase with robust proteolytic activity []. Co-transfection of all four, but not any three, components of human γ-secretase yielded high expression levels. This observation strongly suggests the co-folding nature o
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FPR family Human FPR was
2021-12-28

FPR family Human FPR was first defined biochemically, in 1976, as a high affinity binding site on the surface of neutrophils for the prototypic N-formyl peptide formyl-methionine-leucyl-phenylalanine (fMLF). It was then cloned in 1990, by Boulay et al. from a differentiated HL-60 myeloid leukemia-c
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Reports described a range of
2021-12-28

Reports described a range of synthetic GPR40 agonists with desirable safety and efficacy profiles, compared with existing antidiabetic therapies such as insulin and sulfonylureas [[20], [21], [22], [23], [24], [25], [26], [27], [28]]. Among them, several small molecules were tested in the clinical t
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br Experimental procedures br Results Hdc
2021-12-28

Experimental procedures Results Hdc-KO mice show basal activation of the MAPK and AKT/GSK3β pathways in the dorsal striatum (Rapanelli et al., 2014). These signaling pathways are differentially regulated by the H3 receptor in dMSNs and iMSNs in wild-type mice (Rapanelli et al., 2016). To bette
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Similarly towards the acylsulfamoyl benzoxaboroles the boron
2021-12-28

Similarly, towards the 5-acylsulfamoyl benzoxaboroles, the boronate intermediate was prepared according to , while the boronate , an intermediate towards 4-acylsulfamoyl benzoxaboroles, was prepared according to . The sulfonamides and used in the synthesis were made from the starting sulfonyl chlori
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HBV is an enveloped double stranded DNA virus
2021-12-28

HBV is an enveloped, double-stranded DNA virus, which is transcripted into four major transcripts [6]. Among them, the 3.5 kb pregenomic RNA (pgRNA) directs the translation of HBV polymerase, core protein and acts as template for reverse transcription. So viral transcription is a key step of virus l
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