Archives
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To investigate the mechanism of action of trisubstituted azo
2021-04-19
To investigate the mechanism of action of 2,4,5-trisubstituted azoles, we profiled selected 2,4,5-trisubstituted azoles against a panel of 97 kinases to identify potential targets that could be involved in cardiogenesis. We narrowed down the identified targets to the casein kinase 1 (CK1) family due
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In the literature we can
2021-04-19
In the literature, we can find two different modes of action for estrogens: Firstly there is the commonly accepted genomic pathway. Estrogens pass the cell membrane due to their lipophilic character via diffusion and bind to estrogen receptors (ERs) in the cytoplasm. After binding a dimerization of
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Studies have recently raised concerns about the potential ro
2021-04-19
Studies have recently raised concerns about the potential role of parabens in breast cancer, as these chemicals are commonly detectable in human breast cancer tissues. An analysis of 160 breast tissue samples collected from 40 mastectomies for primary breast cancer in England showed that at least on
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The requirement for two distinct
2021-04-19
The requirement for two distinct signalling pathways for cAMP-induced growth arrest likely represents an important mechanism allowing VSMC to finely modulate their cellular responses to cAMP-elevating stimuli. Our data demonstrates for the first time that activation of both pathways in VSMC results
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Recoverin is a kDa retinal protein that binds
2021-04-19
Recoverin is a 23-kDa retinal protein that binds to calcium. It regulates the Palomid 529 of rhodopsin during visual transduction within photoreceptor cells. Since the pathogenicity of anti-recoverin antibody is potent, anti-recoverin CAR patients often have progressive visual impairments, characte
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br Introduction Schistosomiasis one of the major parasitic
2021-04-19
Introduction Schistosomiasis, one of the major parasitic diseases that affect humans in tropical and subtropical countries, is an acute and chronic condition caused by blood flukes (trematode worms) of the genus Schistosoma (World Health Organization, 2014). Schistosomiasis infects over 240 milli
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br EBI structure and expression The gene
2021-04-19
EBI2 structure and expression The gene encoding EBI2 was originally identified together with EBI1 (CCR7) as the most highly upregulated gene in Epstein–Barr virus-infected Burkitt's lymphoma cells [18]. EBI2 belongs to the rhodopsin-like subfamily of seven transmembrane GPCRs [19]. Although it is
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br The classical ubiquitination pathway Ubiquitination is an
2021-04-19
The classical ubiquitination pathway Ubiquitination is an enzymatic process that involves the addition of an ubiquitin protein to a substrate that usually becomes inactivated followed by degradation in the proteasome; however, several other functions have also been described. For the discovery of
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Subgroup analysis showed that patients with relatively
2021-04-19
Subgroup analysis showed that patients with relatively lower CrCl levels (>50–80 mL/min) were more likely to initiate treatment on a lower dose (17% for all DPP-4 inhibitors; 22% excluding linagliptin). Nevertheless, even in patients with higher CrCl value (>80–120 mL/min and >120 mL/min), at least
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Eleutherococcus senticosus Rupt Maxim Maxim is a shrub belon
2021-04-19
Eleutherococcus senticosus (Rupt. & Maxim.) Maxim is a shrub belonging to the Araliaceae, which is commonly distributed in China, Korea, Japan and Russia. It has been traditionally used as folk medicine for the treatment of rheumatism, diabetes, and hepatitis (Nan et al., 2004). Recent phytochemical
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The effect of NAT deletion on mitochondrial function
2021-04-19
The effect of NAT1 deletion on mitochondrial function in MDA-MB-231 PFTα has been reported elsewhere (Carlisle et al., 2018). However, unlike the data presented here, increases in reserve capacity and glycolytic reserve were seen. The reasons for this variance between our study and that of Carlisle
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Almost of drugs in the market undergo deactivation though ox
2021-04-17
Almost 75% of drugs in the market undergo deactivation though oxidation, reduction or hydrolysis by cytochrome P450 (CYP) enzymes, and then, either directly or by facilitated excretion from the body (Guengerich, 2008). The CYP3A subfamily is of particular interest because of its broad substrate spec
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br Acknowledgements We thank Jeffrey D Konowalchuk
2021-04-17
Acknowledgements We thank Jeffrey D. Konowalchuk and John Sony Robbins for their technical assistance. This work was supported by Natural Sciences and Engineering Research Council of Canada (NSERC) grants to DRB (RGPIN-2013-355303) and MB (RGPIN-2014-96395). AMR was supported by NSERC Vanier Doct
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br Agonist binding ETA activation is promoted by binding
2021-04-17
Agonist binding ETA activation is promoted by binding of the endogenous peptidergic agonists to their orthosteric binding site on the receptor. ET1 and ET2 (Trp6-Leu7-ET1) bind with equal high affinity to ETA, whereas the third endogenous isopeptide ET3 (Thr2-Phe4-Thr5-Tyr6-Lys7-Tyr14-ET1) binds
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A number of chemical strategies have been developed to desig
2021-04-17
A number of chemical strategies have been developed to design activatable optical imaging probes and have been summarized in several excellent reviews 11., 12., 13., 14., 15.. Fluorogenic enzyme substrates are one of the most explored activatable probe types for enzyme detection. These probes contai