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Using HPLC and an amino acid sequencer the
2020-09-25
Using HPLC and an amino selonsertib sequencer, the site of cleavage into the fluorogenic substrate AbzFRQEDDnp, determined as specific to the endopeptidase STH2, was analyzed and identified as being R2-Q3, and into substrate AbzFGQEDDnp, determined as specific to SH1, it was G2-Q3 (Fig. 5, Fig. 6).
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br Materials and Methods br
2020-09-25
Materials and Methods Acknowledgements Introduction The discoidin domain receptors, DDR1 and DDR2, are two closely related receptor tyrosine kinases (RTKs) that contain a discoidin (DS) homology domain in their extracellular regions. The DDRs were initially discovered by homology cloning ba
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The total reduced glutathione content was determined in both
2020-09-25
The total reduced glutathione content was determined in both 22 9 to examine whether retinol was decreasing glutathione concentrations and thus decreasing the conjugation of NAPQI. Total hepatic (3.9±0.3 vs 4.9±1.0 μmol/g, retinol vs untreated, respectively) and renal (0.4±0.1 vs 0.2±0.1 μmol/g, re
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br Mechanisms of acquired resistance to
2020-09-25
Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may
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br Rationale and hypothesis To discover
2020-09-25
Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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In an effort to discover additional GPCRs directing the
2020-09-25
In an effort to discover additional GPCRs directing the migratory events of responding B cells, we identified Epstein-Barr virus (EBV)-induced gene 2 (EBI2) as a promising candidate. The gene encoding EBI2 (Ebi2, also known as Gpr183) was originally identified together with Ebi1 (Ccr7) as the most h
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br Acknowledgments br Introduction Inflammation is the prote
2020-09-25
Acknowledgments Introduction Inflammation is the protective reaction of the body to infection, injury, or irritation with the aim to remove harmful stimuli such as pathogens, damaged cells, or allergic irritants and to initiate the healing process. Inflammatory abnormalities play a crucial rol
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br Significance Our understanding of the ubiquitin biology h
2020-09-25
Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio
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The number of DBH alleles affects dopamine and norepinephrin
2020-09-25
The number of DBH Amrubicin affects dopamine and norepinephrine levels in the prefrontal cortex of mice when they are treated with disulfiram (33). Disulfiram increased dopamine and decreased norepinephrine levels in their prefrontal cortex of mice with two normal alleles, whereas disulfiram showed
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Poxviruses have double stranded DNA
2020-09-25
Poxviruses have double-stranded DNA (dsDNA) genomes, yet they replicate within the cytoplasm. Poxviruses that cause human disease include monkeypox virus (Reynolds et al., 2004), molluscum contagiosum virus (Hanson and Diven, 2003) and variola virus (VARV), the cause of smallpox, a disease eradicate
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br The DDR kinase domain The DDR intracellular kinase
2020-09-24
The DDR1 kinase domain The DDR1 intracellular kinase domain shares the typical structure of other kinase domains (Fig. 1). However, how DDR1 kinase is activated upon collagen binding is poorly understood. It is thought that the process is fundamentally different from the accepted paradigm of liga
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Our recent discovery M P H R A
2020-09-24
Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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Because flavonoids are widely considered to contribute to
2020-09-24
Because flavonoids are widely considered to contribute to health benefits in humans, including anti-inflammatory, antibacterial, antiviral, anticancer, antiplatelet properties, and free radical scavenging capacity (Xiao et al., 2011), efforts have frequently been made to increase their bioavailabil
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Immunofluorescence Cells were fixed with paraformaldehyde PF
2020-09-24
Immunofluorescence. Cells were fixed with 4% paraformaldehyde (PFA) in PBS and extracted by 0.5% Triton X-100-PBS, or fixed in cold methanol. The cells were immunostained with mouse monoclonal LDN193189 Hydrochloride against α-tubulin (Sigma), γ-tubulin (Sigma), Ran (Upstate), rabbit polyclonal ant
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The small GTPase Ran regulates karyopherin cargo interaction
2020-09-24
The small GTPase Ran regulates karyopherin–cargo interactions and the directionality of karyopherin-mediated transport. Like other Ras-family GTPases, Ran cycles between GTP- and GDP-bound states, and the two surface loops in Ran, referred to as the switch I and switch II loops, undergo significant
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