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Another potential source of variable affinities is inherent
2021-06-21
Another potential source of variable affinities is inherent in the method of RBA determination. While several reports simply use relative IC50 values as RBAs [11], [12], [13], [14], [15], these are only an approximate measure of relative affinity since IC50 varies due to experimental and biological
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In rodent models the loss of
2021-06-21
In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an AICAR phosphate receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitric oxide synthas
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An Ubl modification requires several
2021-06-19
An Ubl modification requires several steps that are catalyzed by three enzymes, referred to as E1 (activating enzyme), E2 (conjugation enzyme), and E3 (ligase). The SUMO E1 is a heterodimer of SAE1 and Uba2 (also known as SAE2). In brief, an Ubl is first activated by E1 through ATP hydrolysis and fo
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The development of C S mutation has been
2021-06-19
The development of C797S mutation has been reported in vivo in a small cohort (15 subjects) of EGFR T790M positive patients progressing after Osimertinib: this tertiary mutation was found, using a droplet digital PCR (ddPCR) assay, in 40% of patients after AR to this agent, while 33% of the cases ex
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In conclusion we have shown that the cellular effects produc
2021-06-19
In conclusion, we have shown that the cellular effects produced by SFN in NSCLC 939 receptor are largely mediated by SFN-induced production of ROS. Cells with higher levels of EGFR were more resistant to SFN treatment and showed resistance to SFN-induced apoptosis, suggesting that high EGFR levels
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The findings of Qiu et al
2021-06-19
The findings of Qiu et al. (2016) represent the first instance of a Ub-specific mono-ADP-ribosyltransferase, as well as the first documentation of E1/E2 independent ubiquitination. Post-translational modification of Ub certainly adds layers of complexity to our understanding of the Ub signal and sho
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The compounds were ranked based on the Glide XP
2021-06-19
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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In contrast to chordates authentic chemokine and receptor or
2021-06-18
In contrast to chordates, authentic chemokine and receptor orthologues can be found in the agnathan fishes (Bajoghli, 2013, Kuroda et al., 2003, Nomiyama et al., 2011, Nomiyama et al., 2013); sea lamprey has at least five chemokine receptor genes, one CXCR4 (Ensembl Acc. No.: ENSPMAP00000007678) (Ku
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It was recently reported that a functional single
2021-06-18
It was recently reported that a functional single nucleotide polymorphism (rs75932628) within Triggering receptor expressed on myeloid Nalidixic acid 2 (TREM2) is associated with AD (Guerreiro et al., 2013). Homozygous loss of function mutations in TREM2 are also associated with an autosomal recess
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We have previously reported the characterization of A a nove
2021-06-18
We have previously reported the characterization of A-127722, a novel, non-peptide endothelin antagonist that displays very high affinity binding (K=69 pM) with a more than 1000-fold greater affinity for human endothelin ETA than ETB receptor. Although A-127722 is >1000-fold more selective for endot
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It remains unclear how LINE RNA Nucleolin
2021-06-18
It remains unclear how LINE1 RNA-Nucleolin-Kap1 are targeted to the Dux cluster. LINE1-Nucleolin-Kap1 may have other interacting partners with DNA binding specificity. For example, YY1 has been implicated in targeting a repressive complex containing Nucleolin to the human DUX4 cluster (Gabellini et
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br Experimental procedures br Results Fluorescence attributa
2021-06-18
Experimental procedures Results Fluorescence attributable to GnRH-eGFP neurons was observed through the diagonal band of Broca, to the POA of the hypothalamus in GnRH-eGFP transgenic rats for all groups as described previously (Kato et al., 2003, Tada et al., 2013). Discussion The mEPSCs w
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In the present study promoting
2021-06-18
In the present study, promoting bile sr9009 synthesis by activating EP4 receptors was shown to exert protection against hepatic steatosis. This finding may be relevant for treatment of non-alcoholic fatty liver disease, a major cause of liver disease and prominent indication for liver transplantati
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br Regulation of cadherin switching The
2021-06-18
Regulation of cadherin switching The downregulation of E-cadherin during cadherin switching is induced by multiple mechanisms, including methylation of the E-cadherin promoter and signaling pathways that activate E-cadherin-suppressing transcription factors [[61], [62], [63]]. During the progress
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br Abbreviations br Introduction br Collagen induced DDR act
2021-06-18
Abbreviations Introduction Collagen-induced DDR activation A key feature of DDRs is their ability to bind both fibrillar and non-fibrillar collagens (Shrivastava et al., 1997, Vogel et al., 1997). DDR1 and DDR2 recognize the GVMGVO (O, hydroxyproline) motif within fibrillar collagens I–III
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