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GNE-617 Thyroid hormone triiodothyronine T and its precursor
2022-06-14

Thyroid hormone 3,5,3′-triiodothyronine (T3) and its precursor, thyroxine (T4), are iodinated compounds, which are known to regulate the expression of genes involved in various biological processes, such as development, growth and metabolic control. The iodothyronine deiodinase types I, II and III (
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br Materials and methods br
2022-06-14

Materials and methods Results Discussion Although large-scale purification of homogeneous and functional membrane proteins is challenging, it is essential for biochemical, biophysical and structural characterization. This is particularly true for human P-gp, as its atomic structure has only
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Based on the molecular weights of glutamate
2022-06-14

Based on the molecular weights of glutamate (147.13 g/mol) and MSG (169.111 g/mol), the amount of free glutamate intake obtained in this study was equivalent to 297 mg MSG/d and 370 mg MSG/d for children and adults, respectively. Several previous studies have assessed population intake of MSG from f
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Further explorations at the ortho and meta positions of the
2022-06-14

Further explorations at the ortho- and meta-positions of the phenyl in the tail proceeded on the basis of the preliminary results. First, we investigated the fluorine group at the meta- (13p) and ortho-positions (13q) of the phenyl group, with both compounds being slightly less potent than 13o. Surp
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A oligomers increased ubiquitination of GLT in astrocytes
2022-06-14

Aβ1-42 oligomers increased ubiquitination of GLT-1 in astrocytes. Previous studies found that astrocytic GLT-1 is internalized from the cell surface by ubiquitination of lysines located in the cytoplasmic C-terminus of the transporter (Gonzalez-Gonzalez et al., 2008, Martinez-Villarreal et al., 2012
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To directly address whether pharmacological attenuation of p
2022-06-14

To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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5z br Introduction The growth hormone secretagogue receptor
2022-06-14

Introduction The growth hormone secretagogue receptor (GHSR) gene, which was first isolated from rats and humans (Kojima et al., 1999), comprises two exons and one intron in mammals and chicken. The pig GHSR is located on chromosome 13 (range 110,981,465–111,006,149 on Reference Sscrofa11.1). Alt
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Next we investigated the transfer
2022-06-14

Next, we investigated the transfer of peptides and proteins between contacting cells by nano-LC-MS/MS analysis using the fractions corresponding to molecules higher than 3 kDa. The MS data analysis revealed the direct transfer of several labelled peptides between receivers and donors. Labelled pepti
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The knowledge that piroxicam competes with
2022-06-14

The knowledge that piroxicam competes with ligands that bind to FPR may be of importance for a deeper understanding of the anti-inflammatory effects possessed by this NSAIDs. It has recently been reported that not only phagocytes but also platelets express FPR on their cell surface and that these re
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FFAs are essential nutritional molecules that can also
2022-06-14

FFAs are essential nutritional molecules that can also modulate numerous cellular functions. Fatty OSMI-1 derivatives like prostaglandins, leukotrienes lysophosphatidic acid, spinhgosine-1-phosphate and others are well documented to carry out signal transduction via G-protein coupled receptors (GPC
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br Promotion of GLS expression
2022-06-14

Promotion of GLS2 expression Glutamine metabolism is another target for alteration in ferroptosis. Glutamine is required for the induction of ferroptosis during serum-induced injury after amino TC-I 15 receptor starvation [72]. The first step of glutamine catabolism is its conversion to glutamat
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During the activation of the coagulation cascade factor Xa F
2022-06-14

During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium CM-272 on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit platele
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Here we employ a genetic
2022-06-14

Here we employ a genetic approach to examine the potential interaction of Gli3 and Ezh2 with respect to anteroposterior limb bud polarity. Loss of Ezh2 in a Gli3 mutant background leads to synergistic loss of anterior identity, although the double mutant phenotype more closely resembles that of Ezh2
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br Transportation from TGN toward plasma membrane The insuli
2022-06-14

Transportation from TGN toward plasma membrane The insulin molecules are packaged along with other molecules such as C-peptides, amylin, Zn2+, ATP and GABA in synaptic-like macrovesicles (SLMVs, with the diameters of 50–100 nm) and large dense core vesicles (LDCVs, with the diameters of 200–500 n
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Acknowledgments The authors would like to thank members
2022-06-14

Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD
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