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The transcription factor Nrf is a master regulator of cytopr
2021-11-06

The transcription factor Nrf2 is a master regulator of cytoprotective responses to endogenous and exogenous stresses caused by reactive oxygen species (ROS) and electrophiles [6]. Nrf2 promoter polymorphisms are significantly associated with the development of gastric mucosal inflammation, either in
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As evidenced by SARs and crystallographic data HO has
2021-11-06

As evidenced by SARs and crystallographic data, HO-1 has at least three main crucial regions for inhibitor binding. The most crucial area, the so-called eastern region, is able to allocate the azole ring that represents the first anchoring point by establishing a coordination binding to the heme fer
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br Materials and methods br
2021-11-06

Materials and methods Results Discussion Myocardium reperfusion injury contributes almost half of myocardial infarct size in myocardial infarction patients, and infarct size is closely correlated with the probability of developing amprenavir failure [1]. Despite this knowledge, myocardial
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The NF B family of
2021-11-05

The NF-κB family of transcription factors is involved in acquisition of resistance to anticancer drugs as well as to apoptosis. NF-κB-mediated mdr1 gene upregulation is part of the anti-apoptotic protection mechanism of proximal tubule (PT) clobetasol price against cadmium-induced oxidative stress
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Tamoxifen is still the most frequently
2021-11-05

Tamoxifen is still the most frequently used selective estrogen receptor mediator (SERM) in premenopausal women suffering from estrogen receptor positive (ER+) breast carcinomas [15]. Although this therapy has been proven very successful, about 20–30% of ER+ breast tumors will not respond, or acquire
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The simple carrier model for GLUT
2021-11-05

The simple carrier model for GLUT1 transport activity proposes that the transporter alternates between an outward facing glucose binding site and an inward, cytoplasmic, facing glucose binding site. Cytochalasin B is an endofacial inhibitor and appears to preferentially bind to the open, inward faci
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Work in the Ruiz i Altaba lab was funded by
2021-11-05

Work in the Ruiz i Altaba lab was funded by grants from the Swiss National Science Foundation, the Ligue Suisse Contre le Cancer, the European FP7 Marie-Curie Initial Training Network HEALING, a James McDonnell Foundation 21st Century Science Initiative in Brain Cancer-Research Award and funds from
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In the small intestine digestion and absorption of
2021-11-05

In the small intestine, digestion and Cholera Toxin of the nutrients are the next processes with an impact on the resulting plasma profile. Normally, neither carbohydrate digestion nor absorption are limiting factors, which is illustrated by the rapid and extensive absorption of glucose in conditio
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From a cell signaling perspective given the
2021-11-05

From a cell signaling perspective, given the importance of agonist-directed signaling and biased agonism, one goal of this research update was to review the known contributions of G protein-dependent versus β-arrestin-dependent signals toward promotion of beneficial functions that FFA4 facilitates.
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MMV s distinct mode of inhibition addresses
2021-11-05

MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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Our data show that oxidative stress
2021-11-05

Our data show that oxidative stress (high levels of ROS) suppresses the process of lysosomal exocytosis, which would be predicted to impair the expulsion of toxic compounds from cells. Therefore, we propose that ROS have a biphasic effect on the lysosomal clearance: consistent with their role as a s
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Following the discovery of diketo compounds S
2021-11-05

Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent gssg based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioassay
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Evidence demonstrating the interplay between hypoxia and
2021-11-05

Evidence demonstrating the interplay between hypoxia and the dynamics of histone methylation is mounting [15], [43]. For example, hypoxia leads to an increase in H3K4me3 by inhibiting their responsible demethylase [44]. Hypoxia also leads to an increase in H3K9me2 by upregulating the methyltransfera
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In summary we have provided evidence that TA
2021-11-05

In summary, we have provided evidence that TA, a novel HATi, inhibits the acetylation of histone and non-histone proteins and activation of the mRNA expression of lipogenesis-related genes both in vitro and in vivo (Figure 8), indicating that inhibition of HAT activity by TA is necessary for the pre
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Evidence indicates that astrocytes play a role in the modula
2021-11-05

Evidence indicates that astrocytes play a role in the modulation of NMDAR activity in the CA1 (Henneberger et al., 2010; Papouin et al., 2017a, Papouin et al., 2017b; Robin et al., 2018). Therefore, we sought to examine whether astrocytes are involved in the H1 receptor antagonist/inverse agonist-in
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