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Targeting the MAPK pathway has attracted significant
2020-12-24
Targeting the MAPK pathway has attracted significant interest in cancer therapy. Efforts directly targeting RAS protein are believed to be very challenging in spite of the promise shown by a few RAS inhibitors in the early development stage. Clinical benefits achieved by BRAF and MEK inhibitors have
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Methods br Results First we compared A plaque number A
2020-12-24
Methods Results First, we compared Aβ plaque number, Aβ concentration, and neurobehavior functions between naive APP/PS1 and APP/PS1xEP1−/− mice. Significantly lower Aβ burden in APP/PS1xEP1−/− mice was evidenced by fewer plaques in the hippocampal area and a lower concentration of soluble Aβ42
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Conventional assays rely on a comparable transformation of t
2020-12-24
Conventional assays rely on a comparable transformation of the target analytes and the structurally similar (but not identical) proxy substrates and are commonly used to measure individual enzyme activities in (pre-treated) intact sludge flocs (Burgess and Pletschke, 2008a, Gessesse et al., 2003, Yu
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br Introduction As a serine proteinase and a
2020-12-24
Introduction As a serine proteinase and a sub-family of the chymotrypsin-like proteinase, Glutamyl endopeptidase (GE), which is mainly found in Bacillus species, specifically cleaves negatively charged amino vx 809 residues (Glu/Asp) (Yokoi et al., 2001). Madsen et al. (Madsen & Qvist, 1997) rep
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In vitro studies in NSCLC cell lines expressing
2020-12-24
In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC SAR405838 receptor with Growth inhibition (GI50) values ranging from 7 to 32
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br Experimental Procedures br Acknowledgments
2020-12-24
Experimental Procedures Acknowledgments We thank S. Tangye and A. Swarbrick for helpful discussions and critical reading of the manuscript; K. Wood, T. Camidge, and V. Turner for technical assistance; C. Brownlee for cell sorting; the staff of the Garvan Institute Biological Testing Facility f
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Cy5 azide In addition to tissue resident stromal and myeloid
2020-12-24
In addition to tissue-resident stromal and myeloid cell populations, ILCs also readily engage in positive-feedback loops with myeloid Cy5 azide recruited from the circulation. TNF-α produced by inflammatory monocytes recruited to the lungs of mice infected with Klebsiella pneumoniae markedly increa
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In contrast to inflammatory cytokines
2020-12-24
In contrast to inflammatory cytokines, TGF-β has immunosuppressive properties yet is also important for tissue imprinting immune cell function during development [23]. Salivary gland (SG) ILCs, in addition to liver and intestinal intraepithelial ILC1, express markers denoting tissue residency and TG
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br A brief history of RBR E s RBR E
2020-12-24
A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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Due to the high attractiveness of E and E
2020-12-24
Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), 8-pCPT-2-O-Me-cAMP-AM mg (Davydov et al., 2004, Huang et al., 2005, Kenten et
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Several DA receptors heteromers with a therapeutic
2020-12-23
Several DA receptors heteromers with a therapeutic potential have been described, including D1R/D3R (Fiorentini et al., 2010), but their roles remain to be established. Moreover, most studies on receptor heteromers in addiction focused on the striatum because of its key role in the pathology and its
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Introduction Amphetamine AMPH methamphetamine MA and ethylen
2020-12-23
Introduction Amphetamine (AMPH), methamphetamine (MA), and 3,4-ethylenedioxymethamphetamine (MDMA) are widely abused psychoactive substances, with the basic chemical structure of phenylethylamine [1]. The abuse of these drugs is associated with psychostimulant, anorectic and hallucinogenic properti
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At this stage it is still difficult to assign specific
2020-12-23
At this stage it is still difficult to assign specific domains to some of the regions observed in these structures, although some attempts have already been made (Brewerton et al., 2004). Clearly, higher resolution data is needed. In the future, even if an atomic structure of DNA-PKcs is determined,
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Preclinical and clinical research indicates that inflammatio
2020-12-23
Preclinical and clinical research indicates that inflammation contributes to the progression of ICH injury. Therefore, there is a pressing need to develop interventions that can limit neuroinflammation and its detrimental effects on hcv virus function. Inflammatory cytokines are secreted in the bra
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Compounds and were synthesized according
2020-12-23
Compounds and () were synthesized according to . Reductive amination of ethyl acetoacetate with aniline afforded ester . Saponification of followed by intramolecular Friedel–Crafts acylation afforded ketone . Amide formation with benzoyl chloride followed by a reductive amination yielded compound
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