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To develop novel EPAC inhibitors Zhou and
2021-05-20

To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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To assess whether the described cooperation between
2021-05-20

To assess whether the described cooperation between the EGFR and FGFR receptors was relevant at the clinical level, we determined the effect on progression-free survival of FGFR1 expression in patients with adenocarcinoma who were receiving erlotinib or gefitinib. As we had observed EGFR-FGFR1 coope
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Downregulation of tumor suppressors is a major factor
2021-05-20

Downregulation of tumor suppressors is a major factor that leads to tumorigenesis. Phosphatase and tensin homolog deleted on chromosome 10 (PTEN), a common tumor suppressor, the p2x receptors of which is often downregulated or even absent in the majority of human cancers, functions as a phosphatase
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br Experimental All starting materials and reagents were
2021-05-20

Experimental All starting materials and reagents were purchased from Sigma-Aldrich, Merck and Loba Chemie. Thin layer chromatography (TLC) was performed on silica gel G60 F254 (Merck) plates and eluted with the mobile phase n-hexane: ethyl acetate (70:30%v/v). Melting points were recorded on auto
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Due to cell cell interactions high concentrations of LTs can
2021-05-19

Due to cell-cell interactions, high concentrations of LTs can be locally generated in a short period of time during an inflammatory response, thus potentiating LT function. The cellular communication can be mediated between immune cells as well as between immune cells other cell types. Several studi
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Some of the psychoactive actions of nicotine are mediated
2021-05-19

Some of the psychoactive actions of nicotine are mediated by the nigrostriatal and mesolimbic pathways (Di Chiara, 2000, Di Chiara et al., 2004). The nigrostriatal pathway originates in the dopaminergic neurons located in the substantia nigra and terminates in the putamen and nucleus caudatus which
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It is interesting that of the control
2021-05-19

It is interesting that of the control groups, female TG controls only had significantly higher MB-COMT protein than non-TG male controls (Supplemental Table 9, P = 0.005), while these two groups have almost equal expression of S-COMT protein (8.54- vs. 8.34-fold) and their COMT enzyme activity is al
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BDS I Using characteristic features of ECM
2021-05-19

Using characteristic features of ECM proteins and a computational pipeline combining interrogation of protein and gene databases, we previously defined the matrisome as the ensemble of ECM and ECM-associated proteins [[16], [17], [18]]. In mammals, the matrisome represents 4% of the genome, or appro
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Recently pharmacological studies have revealed that natural
2021-05-19

Recently, pharmacological studies have revealed that natural compounds achieve increasing attention due to its high therapeutic effectiveness and low adverse effect, compared with the chemically synthesized compounds. Emodin is a kind of natural anthraquinone derivative enriched in traditional Chine
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Objective Introduction The physiological significance of hyp
2021-05-19

Introduction The physiological significance of hypoxia is undisputed, although largely over looked in the cancer therapeutics field focused on DNA-damage induced by ionizing radiation or drug treatment. Regions of hypoxia occur during a range of diverse biological situations including embryogenesis
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br Acknowledgements br Introduction L Rhamnosidases EC are g
2021-05-19

Acknowledgements Introduction α-L-Rhamnosidases (EC 3.2.1.40) are glycosyl hydrolases (GHs) that cleave terminal α-l-rhamnose from a large number of natural products [1]. The action of α-L-rhamnosidases (α-RHAs) has been reported, among others, on different complex substrates such as heteropol
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Introduction Glucose is the major carbon source in
2021-05-19

Introduction Glucose is the major carbon source in most organisms. Cancer Protease Inhibitor Cocktail (EDTA-Free, 100X in DMSO) in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditi
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Ultrasound is an acoustic wave with a frequency
2021-05-19

Ultrasound is an acoustic wave with a frequency >20 kHz that needs a medium to propagate [20]. Accompanied by the spread of an ultrasonic wave, a series of alternating cycles of compression and rarefaction emerge in the liquid medium. During the rarefaction cycle, microbubbles are formed because of
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br Results and discussion The effects of hypoxia a
2021-05-19

Results and discussion The effects of hypoxia, a combination of shear stress and hyperoxia, and a combination of shear stress and hypoxia in BAECs were assessed at 0, 15, 30, 60, 120, and 180 min. Changes in phosphorylation levels of eNOS at Ser635 were investigated using immunoblotting, and repr
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br RING dimerization RING type domains are found in many
2021-05-19

RING dimerization RING-type domains are found in many different structural contexts. While many exist as single-chain Z-FA-FMK (Fig. 3A), a notable feature of RING-type E3s is their tendency to form homodimers and heterodimers (Fig. 3C–F). Homodimeric RING-type E3s include cIAP, RNF4, BIRC7 (show
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