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A combination of factors might however account for
2024-03-05

A combination of factors might, however, account for the low rate of success of drug development for neuropsychiatric disorders. First, in most neuropsychiatric disorders, the symptomatology is heterogeneous and the neurobiology remains poorly understood, making therapeutic targets difficult to iden
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The nAChR has been considered an interesting potential targe
2024-03-04

The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none
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br Conclusions br Funding This
2024-02-23

Conclusions Funding This work was supported by a Finnish government subsidy for health science research [grant numbers TYH2012141, TYH 2013218, and TYH 2014216]; the SSAC Foundation [grant numbers SLS-504141 and SLS-693781]; and the Paulo Foundation. The funding sources had no involvement in s
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Therefore VEGF and its receptors are expressed in
2024-02-23

Therefore, VEGF and its receptors are expressed in different organs, including the kidneys, the liver and the Chromocarb [55]. In the human placenta, VEGF is mainly synthesized by cytotrophoblast and Hofbauer cells early in the first trimester, whereas Flk-1 and Flt-1 receptors are expressed throug
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br Under normal physiological conditions the agonist binds
2024-02-23

Under normal physiological conditions, the agonist binds to AT1R on the surface of the plasma membrane and activates the receptor, mediating downstream signaling. Then, activated AT1R is phosphorylated by protein kinase C (PKC) [13] or G protein coupled receptor kinases (GPKs, such as GRK2 [13], G
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Based on the general structure function principle in biology
2024-02-23

Based on the general structure-function principle in biology [[19], [20], [21]], toxic oligomers are expected to have well-defined three-dimensional structures to carry out their pathological functions. A common amyloid toxicity mechanism also suggests that toxic oligomers of different amyloid prote
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The glutamate receptors are important to the
2024-02-23

The glutamate receptors are important to the glioma Medroxyprogesterone acetate from escaping the excitotoxicity under physiological conditions. There are three subtypes of ionotropic glutamate receptors, including NMDA, kainate, and AMPA receptors, which are relating to diverse Ca2+ permeability.
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Regarding A Rs and A ARs basal
2024-02-23

Regarding A1Rs and A2ARs, basal conditions generate a low tone of endogenous adenosine and cause A1R activation, in contrast to situations of increased adenosine where A2AR activation becomes dominant. When adenosine concentrations rise, e.g. during hypoxia, also time appears likely important in reg
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To help ensure the fidelity
2024-02-23

To help ensure the fidelity of mitosis and cytokinesis cells monitor these processes and delay cell cycle progression in response to certain defects. The spindle assembly checkpoint (SAC) is a surveillance system which delays s3i onset until a bipolar spindle has been correctly assembled (Lara-Gonz
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IC values were obtained for
2024-02-23

IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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AG-126 br Dysregulated aromatase expression the link between
2024-02-23

Dysregulated aromatase expression: the link between obesity and breast cancer Obesity has been associated with abnormally high expression of the enzyme aromatase in the breast, influencing the local production and bioavailability of estrogens (Morris et al, 2011, Subbaramaiah et al, 2012). Bowers
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br Duality of interest br
2024-02-22

Duality of interest Contribution statement Acknowledgments Introduction Rapid, cell surface-initiated steroid actions have been reported for all major groups of steroid hormones and our understanding of membrane-mediated steroid actions has progressed rapidly over the last two decades. M
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Voreloxin Hydrochloride br Experimental section br Abbreviat
2024-02-22

Experimental section Abbreviations PSA, puromycin–sensitive aminopeptidase; APN, aminopeptidase N; AML, acute myeloid Leukemia; ALL, acute lymphoblastic leukemia; AADR, amino Voreloxin Hydrochloride deprivation response; PAN, puromycin aminonucleoside; DCC, dicyclohexyl carbodiimide; NHS, N–hy
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AAT enzyme activity was readily
2024-02-22

AAT enzyme activity was readily detected in crude cell-free extracts obtained from berry tissues of all accessions but displayed different substrate selectivities (Fig. 2). Cell-free extracts derived from ‘Muscat Hamburg’ berries showed the highest AAT activity with all alcoholic substrates tested,
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Mt a known to be
2024-02-22

Mt2a, known to be upregulated by ozone (Inoue et al., 2008), was also increased in vehicle-pretreated rats exposed to ozone, however, this effect was markedly reduced by both PROP and MIFE, suggesting that the neuroendocrine response is linked to ozone-induced acute phase protein expression. In huma
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