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br Endocytosis of AdipoR Surface receptor activity may be sh
2023-11-16

Endocytosis of AdipoR1 Surface receptor activity may be shut down by endocytic uptake and subsequent lysosomal degradation of the proteins [20]. Clathrin-dependent endocytosis (CDE) has been extensively studied and internalization from the plasma membrane is mediated through clathrin-coated pits
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Extracellular adenosine acts as a local
2023-11-16

Extracellular adenosine acts as a local modulator of cell function via four adenosine receptor subtypes (A1Rs A2AR, A2BR, and A3R) that are involved in numerous physiological and pathophysiological processes [31]. Each is encoded by a separate gene and has different functions, although with some ove
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The assay performance was estimated using Z factors plotted
2023-11-16

The assay performance was estimated using Z′-factors (plotted in Fig. 2A) according to Zhang et al. calculated for each plate comparing positive (in the absence of an inhibitor) and negative controls (in the presence of an AdK inhibitor). The mean Z′-factor±SD was determined to be 0.7±0.1, indicativ
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Several studies have recently used optogenetics to selective
2023-11-16

Several studies have recently used optogenetics to selectively activate various cholinergic neurons (Jiang et al., 2014). However, most do not explicitly report direct release of GABA from cholinergic fibers, with the exception of our two studies described above (Saunders et al., 2015a, Saunders et
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The obtained results indicate that
2023-11-15

The obtained results indicate that even when the impairment of the same forms of memory are present, amnesia can develop in different ways. Impairment of memory reconsolidation in the conditioned food aversion model through both the serotonin receptor antagonist and the antagonist of NMDA glutamate
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The identification of novel kinase inhibitor
2023-11-15

The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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IC values were obtained for an expanded version of
2023-11-15

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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br Resection of DNA ends
2023-11-15

Resection of DNA ends The highly conserved MRN/MRX complex (Mre11-Rad50-Nbs1 in metazoan; Mre11-Rad50-Xrs2 in yeast) and the Ku70/Ku80 heterodimer (hereafter referred to as Ku) are the first protein complexes to be recruited at DSBs [6]. The presence of Ku and MRN/MRX mediates the recruitment of
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However most of these SBVS studies were focused
2023-11-15

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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mao inhibitors Calcineurin has been established to be a
2023-11-15

Calcineurin has been established to be a ubiquitous Ca2+-activated serine phosphatase in the nervous system (Pyrzynska et al., 2001). It has been reported that the activation of calcineurin protects aromatase from autophagy-mediated protein degradation, implying that calcineurin-dependent dephosphor
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br Acknowledgments br Introduction Cancer is a
2023-11-15

Acknowledgments Introduction Cancer is a deadly disease of uncontrolled cell division and has the potential to invade or spread to other parts of the body and affects normal functioning of the vital organs. Nowadays cancer is considered as leading cause of human death in all over the world and
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We report here the case of a patient
2023-11-15

We report here the case of a patient with probable genetic prion disease with a Creutzfeldt-Jakob disease-like phenotype associated with a rare PRNP E196K mutation who initially exhibited atypical clinical manifestations principally characterized by behavioral abnormalities. Case report An 80-ye
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heme oxygenase br Acknowledgements This work was supported b
2023-11-15

Acknowledgements This work was supported by National Natural Science Foundation of China (Nos. 21376172, 21528601 and 21621004) and the Natural Science Foundation of Tianjin from Tianjin Municipal Science and Technology Commission (Contract No. 16JCZDJC32300). Introduction Alzheimer’s disease
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Our conclusion was confirmed by two experiments The addition
2023-11-15

Our conclusion was confirmed by two experiments. The addition of aminopeptidase-specific inhibitors at high concentrations allowed us to exclude the possibility of substrate hydrolysis by other proteases present in the samples, for example, endoproteases. After the application of inhibitors, we were
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Lorlatinib is an orally active brain penetrant cyclic aminop
2023-11-15

Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F
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