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harmine Our study provides proof of
2021-06-16
Our study provides proof of principle for dimerizing two different E3 ligases as a novel approach to inducing one ligase to degrade the other one. The outcome of ‘ligase versus ligase’ PROTAC-mediated activity might be unpredictable a priori, but could reveal a new mechanism for proximity-mediated h
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In addition to cleaving ubiquitins off modified proteins DUB
2021-06-16
In addition to cleaving ubiquitins off modified proteins, DUBs can also cleave between ubiquitin moieties within a polyubiquitin chain to edit the ubiquitin signal. DUBs employ different strategies to recognize polyubiquitin (Figure 1). DUBs that rely only on interactions on the S1 site tend to be f
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In humans CYP A major
2021-06-16
In humans, CYP3A4/5, major isoforms of CYP3As in the liver, have variants that reduce the enzyme activities [33], [34]. In addition, Werk et al. recently reported the first case of a complete failure of CYP3A enzyme activity due to homozygous loss-of-function mutation of CYP3A4 combined with nonfunc
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In the present study Asian
2021-06-16
In the present study, Asian swamp eel CXCR1a (MaCXCR1a), MaCXCR1b, MaCXCR2, MaCXCR3a, MaCXCR3b, and MaCXCR4 were identified from the Asian swamp eel genome. To explore the features and functions of these CXCRs, we focused on the identification and molecular characterization of MaCXCRs, and 3-Chlorot
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A phenylacetic acid derivative discovered in
2021-06-16
A phenylacetic 25-hydroxyvitamin d3 derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2
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In general accurate results for the prediction of the solubi
2021-06-16
In general, accurate results for the prediction of the solubility in scCO2 + cosolvents using the CPA-EoS were verified. ALD values for each solute (Table 1) varied from 0.04 to 1.5. Few solutes, such as lauric acid, myristic acid, hydroquinone and salicylic acid, presented the highest ALD values. A
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SPR was used to measure
2021-06-16
SPR was used to measure biomolecular kinetic interactions between TERRA G-quadruplex and ligand in the present study. SPR is a widely used method, but cannot tell which specific type of interaction happened. Compounds with similar structures probably have similar mechanism of interaction, while comp
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Multiple technologies exist for analyzing the contents of si
2021-06-15
Multiple technologies exist for analyzing the contents of single cells, including single-cell DNA sequencing, RNA expression analysis, and protein level and activity measurements (Hu et al., 2018; Narrandes & Xu, 2018; Ortega et al., 2017; Wang & Navin, 2015). Single-cell DNA sequencing is generally
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br Acknowledgements br Introduction Endothelial cells consti
2021-06-15
Acknowledgements Introduction Endothelial neurotransmission constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile rol
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The contribution of local ETA and
2021-06-15
The contribution of local ETA and ETB receptors towards heat hyperalgesia induced by inoculation of XC tumor concentration calculation in the paw of mice has been demonstrated by Baamonde and colleagues (Baamonde et al., 2004). Furthermore, using neuropathic and inflammatory nociception models, sev
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Recent studies support the concept
2021-06-15
Recent studies support the concept that dietary metabolites, such as retinoids and AHR ligands, regulate ILC3 function. These metabolites act through intracellular nuclear receptors that function as transcription factors, thereby controlling ILC activity through the stimulation of specific transcrip
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br Results br Discussion Our UbV library was originally
2021-06-15
Results Discussion Our UbV library was originally designed to develop inhibitors of deubiquitinases (Ernst et al., 2013). Recently, we showed that UbVs could exhibit multiple binding modes and mechanisms to modulate HECT E3 activity (Zhang et al., 2016)—one set occupied the HECT domain E2-bind
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In the present work we have investigated the reactivity of
2021-06-15
In the present work, we have investigated the reactivity of N-aryl-N′-hydroxyguanidines 1a–d (see Scheme 1 for structures) with the water-soluble Cu(II) complex 8. Using EPR and UV–Visible spectroscopy, we have shown that the studied N-aryl-N′-hydroxyguanidines 1a–d can bind and transfer electrons t
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Introduction Amphetamine AMPH methamphetamine MA and ethylen
2021-06-15
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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Many studies have found that there
2021-06-15
Many studies have found that there is an aberrant DNA methylation in the imprinting control region of development-related genes in the spermatozoa of oligozoospermic men (Kobayashi et al, 2007, Marques et al, 2004, Marques et al, 2008), which most likely results from expressional changes in the DNMT
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