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Neuropathic animals display increased sensitivity to
2024-07-10
Neuropathic animals display increased sensitivity to the anti-nociceptive effect of baclofen and whilst the number and affinity of GABAB trilithium in the dorsal horn are not altered (Smith et al., 1994; Zemoura et al., 2016), GABAB receptors subunits (B1 and B2) are both down-regulated in sensory
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br Author contributions br Financial disclosures br Acknowle
2024-07-09
Author contributions Financial disclosures Acknowledgements We thank Ms. Eva So for the editorial assistance. This work was supported by grants from the National Natural Science Foundation of China (No. 81622015, 81571042 and 81501143) and the National Basic Research Program of China (No. 2
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Circular dichroism CD provides useful information
2024-07-09
Circular dichroism (CD) provides useful information about protein structure, the extent and rate of structural changes and ligand binding. CD is a form of light gnrh agonist spectroscopy that measures differences in the absorbance of right- and left-circularly polarized light (rather than the commo
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The direction of research then turned to
2024-07-09
The direction of research then turned to investigating the long-term effects of adiponectin on insulin resistance. Adiponectin transgenic mice showed a reduction in insulin resistance and diabetes [5,6], while adiponectin-deficient mice showed mild insulin resistance with glucose intolerance, as wel
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However although in vitro studies in heterologous systems
2024-07-09
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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br Results and discussion The morphology and structure
2024-07-09
Results and discussion The morphology and structure of MI-77301 samples were observed using an SEM, as shown in Fig. 1. The length and thickness of the actin filaments were regulated with ABPs to mimic the various actins observed in cells. We prepared three types of F-actin with or without gelsol
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Prostate cancer is the second leading cause
2024-07-09
Prostate cancer is the second leading cause of cancer-related death in men in the United States [25]. Similar to pancreatic cancer, prostate cancer has few diagnostic options available, particularly to differentiate indolent from aggressive disease. Axl is also overexpressed in ∼50% of prostate canc
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A role for YAP in mediating resistance to EGFR inhibition
2024-07-09
A role for YAP in mediating resistance to EGFR inhibition has also been described [28], [29]. In line with these evidences, we observed increased YAP activation in all the generated EGFR TKI–resistant cells, testified by decreased phosphorylation on the inhibitory serine 127, enhanced nuclear locali
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Oocytes from the African clawed frog
2024-07-08
Oocytes from the African clawed frog Xenopus laevis have been widely used as an expression system to study the modulation of NMDA receptors by metabotropic receptors, such as metabotropic glutamate receptors [12], μ opioid receptors [13], insulin receptors [14] and serotonin receptors [15]. No data
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However most of these SBVS studies were focused on the
2024-07-08
However, most of these SBVS studies were focused on the target(s) for which crystal structures were available or have a similar template in PDB for comparative modeling. Besides, these were limited to SBVS only which relies on the rigid binding pocket, therefore, it may result in high false positive
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Analysis of ASK crystal structures as well as
2024-07-08
Analysis of ASK1 crystal structures as well as an investigation of how AZ505 ditrifluoroacetate mg 4 might bind were undertaken to understand opportunities for engaging Gln756. To this end a docking model derived from PDB 3VW622 was used to predict the binding mode of amide 4 in the ASK1 active sit
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Several MAP kinases are involved in the
2024-07-08
Several MAP kinases are involved in the signal transduction pathways that lead to the upregulations of inflammatory mediators. Moreover, transcriptional activations of STATs are regulated by MAP kinases, as evidenced by reports that p38 MAPK is necessary for the S727 phosphorylation of STATs (Kovari
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Previous research showed that combination of
2024-07-08
Previous research showed that combination of chitosan and MPI-0479605 nanocrystals (CNCs) can produce coating films with superior properties (Naseri, Mathew, Girandon, Fröhlich, & Oksman, 2015). CNCs are crystalline nanometer sized rod-like particles. It has been demonstrated that antimicrobial acti
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There are some limitations and further experiments
2024-07-08
There are some limitations and further experiments that are required. First, to our surprise, measurement of the cardiomyocyte cross-sectional area in Akt1−/−/iAkt2 KO mice showed comparable areas to WT mouse despite of reduced heart weight. In addition to measuring cardiomyocyte cross-sectional are
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Interestingly intermittent high doses of AKT inhibitors have
2024-07-08
Interestingly, intermittent high doses of AKT inhibitors have been shown to be a more effective strategy both clinically and pre-clinically. High doses appear to be required for induction of apoptosis and intermittent schedules overcome the low therapeutic index of these compounds. This is particula
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