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Having taken a step back from affinity to
2024-09-18
Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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br Involvement of LPA receptors in cancer LPA
2024-09-18
Involvement of LPA receptors in cancer LPA׳s effects are mediated by at least six different G protein-coupled receptors (LPA1–6). Human gastric and ovarian cancers overexpress the mRNA encoding LPA1 and LPA2 compared to healthy tissues [6], [11], [12]. Papillary and follicular thyroid cancers exh
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NSC 74859 Loss of virulence in ACL mutants
2024-09-18
Loss of virulence in ACL mutants may be caused by defect in vegetative growth and conidial germination, and reduced trichothecene production. However, supplement of potassium acetate restored the defects in germination rate and vegetative growth, but not virulence in wheat heads (Table 2, Fig. 2B),
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br Materials and methods br
2024-09-18
Materials and methods Results Dried GF 109203X synthesis used were 48.46 g C. benghalensis, 857.98 g T. zebrina and 25.09 g T. fluminensis. The samples gave 12.9% C. benghalensis, 0.078% T. zebrina and 3.06% T. fluminensis methanol extracts. The methanol extracts were evaluated for their lip
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retinoid x receptor The current findings proved that citral
2024-09-14
The current findings proved that citral treatment induced mitochondrial-mediated apoptotic cell death in both HCT116 and HT29 through the p53 and ROS. As such, citral promoted apoptosis as evident by the externalization of PS and dissipation of Δψm at 24h of treatment in HCT116 and HT29 cells. These
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br Conflict of interest br
2024-09-14
Conflict of interest Acknowledgment The authors gratefully acknowledge the financial support from the National Natural Sciences Foundation of China (81070220 and 81170278), and the Aid Program for Science and Technology Innovative Research Team in Higher Educational Institutions of Human Provi
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MADS box proteins are combinatorial transcription factors in
2024-09-14
MADS box proteins are combinatorial transcription factors in that they often derive their regulatory specificity from other DNA binding or accessory factors. In many cases, the cofactor with which MADS box proteins interact specifies which genes are regulated, when they are regulated and if these ge
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br Acknowledgements We thank the National Natural Science
2024-09-14
Acknowledgements We thank the National Natural Science Foundation of China (41576156), Shandong Province Science and Technology Development Plan (2015GSF121045), Yantai Science and Technology Development Plan (2015ZH078), and the Public Science and Technology Research Funds Projects of Ocean (No.
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In receptor binding terminology both
2024-09-14
In receptor binding terminology, both receptor and acceptor contain a receptive site for the ligand, although only the receptor induces a biological function. Moreover, the acceptor lacks an endogenous ligand. Many proteins have been described as receptors for toxic Aβ assemblies, implying a designe
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There is a growing body
2024-09-14
There is a growing body of evidence showing that pentobarbital causes memory disorders [3], [4], [5]. Our results that a single injection of pentobarbital into bilateral hippocampus significantly impaired hippocampus-dependent spatial memory retrieval (Fig. 1) add support to that evidence. Previous
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Following activation of mGluRs GRIP stabilized AMPARs appear
2024-09-14
Following activation of mGluRs, GRIP-stabilized AMPARs appear to be the primary target for endocytosis. Consistent with this model, we find that using siRNA to reduce GRIP1/2 expression blocks the AMPAR internalization and the synaptic depression mediated by mGluRs. Reductions in GRIP1/2 expression,
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br Effects of BCAAs on glucose
2024-09-14
Effects of BCAAs on glucose metabolism Insulin plays an exclusive role in regulation of glucose metabolism, and obesity and type 2 diabetes induce hyperinsulinemia due to insulin resistance. Plasma BCAA concentrations are increased by 14–20% in patients with hyperinsulinemia under overnight fasti
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br Impact of global AHR deficiency on
2024-09-14
Impact of global AHR deficiency on diet-induced obesity Two subsequent studies in which AHR function was affected at the whole animal level corroborated the role of AHR in dietary obesity. Xu et al. [14] showed that on a high-fat diet, both AHR-deficient Ahr−/− and hemizygous Ahr+/− mice gained s
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Given the profound expression of HT A and
2024-09-14
Given the profound Butaprost of 5-HT1A and 5-HT2A in the hippocampal CA1 region, and their potential to complex with mGluRs, the objective of this study was to examine if sleep deprivation alters the expression of 5-HT1A and 5-HT2A receptors and determine whether potential changes are reversible po
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Active SI behavior was dose dependently affected by
2024-09-14
Active SI behavior was dose-dependently affected by PACAP treatment (F3,25 = 14.42, p casin synthesis 1 week later (F3,20 = 8.93, p hypothesis that PACAP causes disruptions in posterror adjustments that are similar to disruptions seen in humans with depression.
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