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The G R mutation is located at the
2024-03-18
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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Whether similar mechanisms play a role in adiponectin signal
2024-03-18
Whether similar mechanisms play a role in adiponectin signal transduction and whether additional proteins are recruited to adiponectin receptors via APPL1 has not been analysed so far. Although it has been clearly established that APPL1 is a downstream adaptor protein in adiponectin signal transduct
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At present drugs that specifically
2024-03-16
At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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Five alternatively spliced isoforms of ATX
2024-03-16
Five alternatively-spliced isoforms of ATX have been described and all are catalytically active [16], [17]. The original ATX described in 1992 is termed ATXα, whereas the most abundant isoform is ATXβ and is the same isoform responsible for plasma lysoPLD activity [18]. Full length ATX is synthesize
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(S)-10-Hydroxycamptothecin To identify the kinase s
2024-03-16
To identify the kinase(s) mediating H3.3S31 phosphorylation, we devised a 96-well-plate-compatible immunostaining assay, with (S)-10-Hydroxycamptothecin specific for H3.3S31ph, and utilized it to screen both a Qiagen siRNA library covering 720 human kinases and a kinase inhibitor library (Selleck)
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br Dysregulated aromatase expression the link between obesit
2024-03-16
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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NLG-8189 On the other hand key enzymes
2024-03-16
On the other hand, key NLG-8189 also involved in NO metabolism are nNOS and eNOS. Apparently, during acute ischemia, eNOS activity and NO concentration surge for a short period of time (Schulz et al., 2004) but eventually the expression and activity of the synthase and consequently NO concentration
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Apelin is a peptide hormone and an endogenous ligand for
2024-03-16
Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid
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Another interesting aspect of neutralizing AP is the
2024-03-16
Another interesting aspect of neutralizing AP-1 is the inhibition of interactions between AP-1 and Smad proteins, which synergize to activate the TGF-β1-responsive genes involved in hypertrophic growth of the heart muscle and in the development of cardiac fibrosis. Through preventing AP-1 activation
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Mass spectrometry Matrix assisted laser desorption ionizatio
2024-03-16
Mass spectrometry. Matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) MS experiment was performed in linear and positive-ion mode on a DE-STR instrument equipped with a nitrogen laser (PE Biosystems, Foster City, CA). Each spectrum was calibrated in the default mode in which 0.1%
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We have shown that an extensive
2024-03-16
We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot
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Evidence from basic science studies suggests that Cd may
2024-03-16
Evidence from basic science studies suggests that Cd may play a role in prostate cancer through disruption of the androgen receptor (AR). AR, a hormone-activated transcription factor, is the key driver of prostate cancer progression [6]. Ironically, the AR is also required for normal prostate growth
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To further demonstrate the significance of Nrf activation in
2024-03-15
To further demonstrate the significance of Nrf2 activation in the prevention of EGF-induced CRC growth by AR inhibitor, we examined the effect of fidarestat on EGF-induced cell viability in Nrf2-ablated cells. Our results suggest that AR inhibitor prevented the EGF-induced cell viability in control
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ion channel Ambient levels of ppm ozone were recorded during
2024-03-15
Ambient levels of 0.2ppm ozone were recorded during a recent 2017 weather event in Texas, United States (EPA, 2007). This concentration or higher levels have been used in several human clinical studies during intermittent exercise (Miller et al., 2016c). Although ozone concentration of 0.8ppm used i
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A correlation analysis was performed to
2024-03-15
A correlation analysis was performed to investigate a possible relationship between serum resistin levels and MG-ADL. We observed a significant relationship between serum resistin levels and MG-ADL scores in AChR-GMG-positive cases (r=0.285, p=0.032; Fig. 1C). There were also significant correlation
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