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The quantification and monitoring of ChEs
2019-09-21
The quantification and monitoring of ChEs enzymatic activities have traditionally been associated to environmental studies in order to diagnose the exposure of non-target organisms to specific anti-cholinesterasic agents (Nunes, 2011). The importance of these enzymes as biomarkers of environmental c
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We have previously reported the characterization of A
2019-09-21
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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Ultrasound is an acoustic wave with a frequency
2019-09-21
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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In terms of its protease activity MME has a
2019-09-21
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other nitric oxide synthase inhibitors of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target an
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br Experimental Procedures br Author Contributions br Acknow
2019-09-21
Experimental Procedures Author Contributions Acknowledgments Introduction Germinal centers (GCs) form in secondary lymphoid organs of vertebrates in response to challenge with T-cell-dependent antigens. After extrafollicular and follicular interactions with cognate antigen and T helper c
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2-Hydroxypropyl-β-cyclodextrin Given the important regulator
2019-09-21
Given the important regulatory roles Ub signaling pathways play in eukaryotes, bacterial pathogens and viruses have evolved elaborate mechanisms to hijack host Ub signaling pathways and evade the immune response. This is highlighted by the numerous E3 Ub ligases and spectrum of DUBs encoded by bacte
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Some family I DNA ligases can use dATP
2019-09-21
Some family I DNA ligases can use dATP as nucleotide cofactor. For instance, human Thioguanine I uses dATP with a catalytic efficiency that is only 36-fold lower in comparison to ATP [9]. EhDNAlig is unable to use dATP as a nucleotide cofactor, indicating a more constrained active site in compariso
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Dgat mice however had less
2019-09-21
Dgat−/− mice, however, had less adipose tissue, as reflected by lower total fat pad weights and body triglyceride content. Because of these findings, we hypothesized that, although Dgat−/− mice could make triglycerides through non-DGAT pathway(s), their triglyceride synthesis capacity might not be e
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Previously published results on this topic are
2019-09-21
Previously published results on this topic are inconsistent. Stressin1-A, a novel CRF1 receptor agonist, increased anxiety-like behavior in the social interaction and shock-probe tests [51]. Pharmacological blockade of CRF1 (NBI-30775) reversed both CRF-induced increases in startle and CRF-induced d
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br Methods Adult male B
2019-09-21
Methods Adult male B6, 129 CRHtklee mice (25–30g at the beginning of the experiments) that were wild-type (CRF1R+/+) and recessive homozygous or knockout (CRF1R−/−) were housed six per cage. Mice were 3–5months old and derived from mating CRF1R+/− breeders (Jackson Laboratory, California). Wild-t
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In recent years there has been much interest within the
2019-09-20
In recent years, there has been much interest within the endothelin community regarding the possibility that ETA and ETB receptors may form homo- and heterodimers. Heterodimerization of endothelin receptors may provide an explanation for the results mentioned in the previous paragraph and might also
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Estrogen related receptors ERRs are orphan nuclear receptors
2019-09-20
Estrogen-related receptors (ERRs) are orphan nuclear receptors and have three members including ERRα, ERRβ, and ERRγ (Yasumoto et al., 2007). Though they are termed as ERRs due to the sequence homology with estrogen receptors, they don’t need to bind estrogens to exert action. Generally, ERRs bind t
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Because of the important role of
2019-09-20
Because of the important role of the DDB1-CUL4B interaction for CUL4B-based E3 ligases, disruption of the DDB1-CUL4B interaction could be an effective approach to treat cancer. Therefore, we developed an in vitro HTS assay based on yeast cell growth inhibition to identify compounds that could disrup
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Extracellular uridine can be transported
2019-09-20
Extracellular uridine can be transported across the cell membrane to enter the nucleotide salvage pathway. A colon cancer cell line supplemented with uridine was capable of growing normally in the presence of 1 μM brequinar (Peters et al., 1992). The supplemented uridine may be transported into the
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br Results br Discussion The structures
2019-09-20
Results Discussion The structures presented here were solved at high sirtuin 1 and show in detail how DDR1 achieves high affinity for imatinib and ponatinib, respectively. Both type II inhibitors bind in their more potent extended conformations to the inactive DFG-out conformation of the kina
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