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The dihydroxynaphthalene derived substrates a a and a Table
2019-09-24
The 2,3-dihydroxynaphthalene-derived substrates 18a, 20a and 22a (Table 2) allowed only moderate growth of all members of the panel of microorganisms suggesting that these substrates were inhibitory to some extent. Strong growth of the Gram-negative microorganisms and moderate growth of the Gram-pos
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Ultrasound is an acoustic wave with a
2019-09-24
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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Two GPCR subtypes of interest in the myocardium are the
2019-09-24
Two GPCR subtypes of interest in the myocardium are the endothelin receptor (ETR) and the α1-adrenergic receptor (α1-AR). Upon ligand binding, these receptors canonically activate the Gαq protein leading to activation of phospholipase C, hydrolysis of phosphatidylinositol 4,5-bisphosphate into diacy
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In mammals neutrophil elastase is a
2019-09-24
In mammals, neutrophil elastase is a trypsin-like serine protease stored in the azurophilic granules of naïve neutrophils [15], [16]. The catalytic activity of neutrophil elastase relies on a His57–Asp102–Ser195 triad (chymotrypsin numbering system) that functions by transfer of electrons from the c
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Despite the differences in the clustering abilities of DDR
2019-09-24
Despite the differences in the clustering abilities of DDR1b versus DDR2 upon ligand administration, we also noted striking similarities in the spatial distribution and phosphorylation of DDR1b-YFP and DDR2-GFP. We show for the first time that in MC3T3-E1 cells, after 4 h of collagen administration,
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Shikonin kinase The AURA trial was a phase I
2019-09-24
The AURA trial was a phase I/II study evaluating the safety, tolerability and activity of Osimertinib in patients with EGFR-mutated NSCLC progressing after a previous EGFR TKI. The phase I component of the study included a dose escalation part (Osimertinib 20mg to 240mg), using a rolling six design,
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Deferiprone In this study we implicate
2019-09-24
In this study, we implicate SCFFBXO3 E3 ligase as a critical modulator of inflammation in atherosclerosis and demonstrate the efficacy of a small molecule FBXO3 inhibitor in suppressing inflammatory responses important in atherosclerosis. Specifically, individuals carrying a hypofunctioning genetic
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Crystallographic and NMR based analyses have revealed that R
2019-09-24
Crystallographic and NMR-based analyses have revealed that RINGs and U-boxes have a common mode of interaction with E2s (Fig. 2A). The key structural elements are two loop-like regions, which, in the case of RINGs, coordinate Zn. The loops surround a shallow groove formed by the central α-helix. Tog
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alln and In the belief that DNA based nanosensors and
2019-09-24
In the belief that DNA-based nanosensors and DNA microarrays should be easier to operate, faster, more accurate and more economically viable than PCR-based techniques, an electrochemical DNA biosensor was designed for detection of G. boninense[9], [10]. This was developed based on a gold electrode m
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BR stimulated PA formation via the DGK
2019-09-24
BR-stimulated PA formation via the DGK pathway might have many effects in regulation of cell metabolism. For example, PA originated from DGKs pathway plays important roles in activation of NADPH oxidases, thus turning on ROS signaling [23]. PA is also connected to regulation of respiration processes
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Beyond phosphorylation cancer cells may alter pyrimidine bio
2019-09-24
Beyond phosphorylation, cancer BKM 120 clinical may alter pyrimidine biosynthesis through the activation of the proto-oncogenic transcription factor MYC. MYC is a master regulator of many different pathways and has significant influence on the expression of nucleotide metabolism genes. Previous stu
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Mitochondrial depolarization induced by DHODH inhibition Fig
2019-09-24
Mitochondrial depolarization induced by DHODH inhibition (Figure 5A) may also contribute to the selective effects of DHODH inhibitors on KRAS mutant cells. If so, the effect may arise more from pro-apoptotic effects of mitochondrial depolarization (Lemasters et al., 1998) than from impaired oxidativ
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Considering the divergence of multiple DGAT
2019-09-24
Considering the divergence of multiple DGAT isoforms, we examined whether MiDGAT1 and MiDGAT2s utilized different fatty acids as the substrate to synthesize TAGs. GC-MS analysis indicated that C16:0 and C18:0 were the major components of TAGs in yeast cells, and all three MiDGATs displayed the same
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DNA damage represents a persistent threat to
2019-09-23
DNA damage represents a persistent threat to genomic stability. A critical link exists between DNA mutation, chromosomal rearrangement and cancer development. In myeloid malignancies, various chromosomal translocations and/or mutations increased cellular reactive oxygen species (ROS), followed by DS
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The large body of structural
2019-09-23
The large body of structural knowledge that is currently available for CRM1 has contributed to atomic level and mechanistic understanding of many steps in the CRM1 nuclear export cycle. However, structural analysis could still inform on several outstanding questions and guide future discoveries pert
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