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br Conflict of interest statement br Introduction Endothelin
2021-05-31

Conflict of interest statement Introduction Endothelins (ETs) are a family of multifunctional, naturally occurring peptides with long-lasting vasoconstrictor and pressor effects (Zhou et al., 2004). They are synthesized as a large protein, the pre-proET-1 or Big ET-1, which is subsequently cle
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A comparative analysis of the cleavage activity
2021-05-31

A comparative analysis of the cleavage activity of different forms of the BoNT/A endopeptidase in reduced conditions with SNAPtide and full-length SNAP-25 substrate is summarized in Fig. 5, Fig. 6. The BoNT/A LC was found to be the most active against SNAPtide, a small peptide segment of the SNAP-25
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br Acknowledgements We would like
2021-05-31

Acknowledgements We would like to thank Dr Ron Mason (NIEHS, Research Triangle Park, NC) for helpful discussion regarding the analysis of CCl4 metabolism, to Dr Karla Thrall and Dr Rick Corley (Battelle) for helpful discussions regarding study design and data interpretation, and to Jim Merdink an
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Interestingly our analyses of human PBMCs using a monoclonal
2021-05-31

Interestingly, our analyses of human PBMCs using a monoclonal antibody against EBI2 showed that the expression pattern of human EBI2 is largely overlapping with that in mice. Especially Th17 AG-126 showed homogeneous high expression of EBI2 compared with Th1 cells, which contained a fraction of cel
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In this study Oncomine GEO and TCGA
2021-05-31

In this study, Oncomine, GEO and TCGA databases were used to analyze the expression of UBE2S gene in HCC and normal liver tissues to determine the relationship between UBE2S expression and prognosis of hepatocellular carcinoma. The potential function of UBE2S in HCC was analyzed by screening UBE2S c
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br Results br Discussion In this paper we present insights
2021-05-31

Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 DY131 via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1 inhibitor
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Next we evaluated whether DPP inhibitor suppressed osteoclas
2021-05-31

Next, we evaluated whether DPP-4 inhibitor suppressed osteoclast formation by downregulating LPS-induced RANKL expression in stromal cells; DPP-4 inhibitor did not inhibit LPS-induced RANKL expression. Furthermore, we evaluated the effect of DPP-4 on LPS-induced RANKL expression in stromal cells, bu
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Consistent with the known tolerance of the
2021-05-31

Consistent with the known tolerance of the Suzuki–Miyaura reaction to a wide range of aryl substituents, we subsequently found that the commercially available 3-hydroxyphenylboronic Furegrelate sodium salt pinacol ester () could be coupled to , to give directly and in comparable yield. Smooth conv
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Z-LEHD-FMK br Materials methods br Results and discussion Th
2021-05-31

Materials & methods Results and discussion The comparison of BFI methods (Table 1) shows that Phosphatesmo failed to detect seminal fluid in all samples. This observation is concordant with other studies that investigated water-exposed seminal fluid stains [6], [7]. The Phosphatesmo test is us
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Finally considering the encouraging inhibitory and selectivi
2021-05-28

Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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Selective inhibitor of phosphodiesterase type
2021-05-28

Selective inhibitor of phosphodiesterase type 5 (PDE5I) is commonly used for ED treatment. PDE5I exhibits its vasodilatory effect by inhibiting the degradation of cyclic guanosine monophosphate (cGMP), which relaxes the smooth muscle and allows increased blood flow for penile tumescence. Udenafil (D
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The ultrafiltration approach has been
2021-05-28

The ultrafiltration approach has been used to measure equilibrium BIEs for a number of enzyme systems, including AEBSF receptor hexokinase (Lewis and Schramm, 2003a, Lewis and Schramm, 2003b), thymidine phosphorylase (Birck & Schramm, 2004), purine nucleoside phosphorylase (Murkin, Tyler, & Schramm
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The development of novel approaches to study
2021-05-28

The development of novel approaches to study GPCR-mediated transactivation in live CGP 42112 is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Grb
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Several main strategies for targeting E s described in
2021-05-28

Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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The HEV vaccine developed based on
2021-05-28

The HEV vaccine, developed based on p239 particles, is of good efficacy, immunogenicity and safety, and was licensed in China in 2012. p239 (aa 368–606) and E2 (aa 394–606) share a common region of ORF2, referred to as E2s (aa 459–606), which harbors the major antigenic determinants of the HEV vacci
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