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The expression of GLUT receptors
2022-10-12

The expression of GLUT receptors throughout the body could be considered a potential source for off-target effects even for engineered glucose-conjugated nanomedicines, as there are at least 12 types of GLUT transporters in the body, including GLUT1 in erythrocytes and the blood-brain barrier, as we
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GKT137831 br Materials and methods br Results
2022-10-12

Materials and methods Results Discussion Defective regulation and inappropriate activation of the HH signaling pathway is implicated in many cancers. SMO targeting inhibitors were the first to enter clinical trials, however complications with acquired resistance and toxicity, also exemplifi
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In addition to the robust
2022-10-11

In addition to the robust intracellular calcium mobilisation, DHA and TUG-891 also induced MMP-9 granules release and superoxide production, supporting a key role of calcium in bovine neutrophil defense responses (Burgos et al., 2011). Pisani et al. (Pisani et al., 2009) described a reduction of bas
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With the nitrogen containing heterocycle components and the
2022-10-11

With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic Losmapimod (, and ), followed by deprotection by TFA, smoothly provided th
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We also evaluated the effect of varying ionic
2022-10-10

We also evaluated the effect of varying ionic strength. These experiments included previously characterized H3 (residues 1–21) and SNAIL (residues 1–9) peptides [8], [34] to allow a comparative analysis with different ligands (Fig. 1A). As shown in Fig. 2 and listed in Table 2, it is evident that a
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br Introduction Local anesthetics LAs are a set
2022-10-10

Introduction Local anesthetics (LAs) are a set of common medicines used for pain management in clinical settings. Up to now, LAs have been extensively used for peripheral nerve blocks, interventional spinal procedures, and epidural anesthesia [1]. In addition to their anesthetic and analgesic eff
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In our previous study we designed and synthesized compounds
2022-10-10

In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic EG00229 australia (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro
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The experiments reported herein were designed to test whethe
2022-10-10

The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, w
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We have previously established the pharmacokinetic profile a
2022-10-10

We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in smad and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The compound CID
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br Pharmacology br Background to GPR function br The
2022-10-10

Pharmacology Background to GPR35 function The emerging function of GPR35 in the nervous system Conclusions The role of GPR35 in the modulation of synaptic transmission, neurogenic and inflammatory pain, and potential signalling pathways involved in these processes are beginning to emerge
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Although it is currently unknown why the longer splice varia
2022-10-10

Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the ASC-J9 receptor splice variant ERbeta2 identified in human and primate, but not other species (Sierens, et
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A high throughput screening campaign
2022-10-10

A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also cont
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WAY 316606 The mammalian AMPA receptor protein family compri
2022-10-09

The mammalian AMPA receptor protein family comprises four subunits, termed GluR-A through GluR-D (or GluR1 through GluR4), which form hetero-tetrameric receptor complexes Dingledine et al. 1999, Rosenmund et al. 1998. These subunits possess distinctive intracellular C-terminal domains that can be gr
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Peripheral injury or disease induced alterations in
2022-10-09

Peripheral injury- or disease-induced alterations in synaptic efficacy occur not only at the first synapse made by the primary nociceptive afferents in the spinal dorsal horn but are also operational in several regions processing the sensorimotor as well as emotional-affective components of pain, su
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As our earlier study investigated
2022-10-09

As our earlier study investigated glut mRNA levels in response to a protein load contained in a meal and the studies that used glucose and insulin injections did not examine GLUT expression, this study sought to investigate the effects of hyperglycaemia and insulin on mRNA levels in the spiny dogfis
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