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br General features of FGFRs and inhibitors br Conclusion
2021-10-29

General features of FGFRs and inhibitors Conclusion Given the critical role of FGFRs in the progression of tumors, the co-crystal structures of these kinases in complex with inhibitors are determined in order to clarify the mechanism of actions and explore new efficient inhibitors. This manusc
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In conclusion a novel series of GPR agonists containing nitr
2021-10-29

In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen LCQ-908 had a remarkable effect on the GPR40 agonistic activity. Co
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C prevents the glutamate and
2021-10-29

C16 prevents the glutamate- and erastin-induced ROS accumulation but does not affect the decrease in GSH, indicating that prevention of ROS accumulation by C16 is not due to the restoration of GSH levels. Instead, C16 itself possessed superoxide anion scavenging activity in vitro at similar concentr
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In humans polymorphisms in the lengths
2021-10-29

In humans, polymorphisms in the lengths of GT sequences (from 11 to 40) within the HMOX1 promoter impact the magnitude of HO-1 expression profiles. Long GT repeats code for less stable (Z-conformational) DNA with blunted transcriptional activity resulting in lower resting and stimulated HO-1 protein
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The transcription factor Nrf is a master
2021-10-29

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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The molecular mechanisms underlying spindle orientation are
2021-10-28

The molecular mechanisms underlying spindle orientation are still largely unknown. Budding yeast has been used to study spindle positioning and asymmetric cell division. Indeed, after cytokinesis, daughter cells have different sizes. The cell division plane is established early in the cell cycle and
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mk-801 Glutathione transferases GST have been discovered in
2021-10-28

Glutathione transferases (GST) have been discovered in many tissues including the cornea of humans and several other mammals (Awasthi et al., 1980, Bilgihan et al., 2003; Gondhowiardjo and van Haeringen, 1993; Saneto et al., 1982, Sastry et al., 1995, Singh et al., 1985, Watkins et al., 1991). To da
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Molecular mechanisms of decidualization have been studied fo
2021-10-28

Molecular mechanisms of decidualization have been studied for years, revealing numerous signaling pathways and transcriptional factors participated in the regulation [37,38]. As a central controller of deicdualization, FOXO1 regulates the transcription of a large number of target genes, which are in
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Historically a role for the prefrontal cortex in
2021-10-28

Historically, a role for the prefrontal cortex in spatial working memory has been repeatedly claimed (for review, see Kolb, 1984). Older studies using traditional, non-fibre-sparing lesions (e.g. aspiration lesions) often resulted in spatial alternation deficits. In contrast, more recent studies emp
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With rare exceptions the biological
2021-10-28

With rare exceptions, the biological role of γ-secretase cleavage of substrates other than Notch 1 has been ignored during proof of concept preclinical repurposing studies. For example, in the GSI AD trial, many individuals noted changes in hair color, apparently due to inhibition of tyrosinase, ano
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Seizures in turn selectively modulate the expression of
2021-10-28

Seizures, in turn, selectively modulate the Ivacaftor benzenesulfonate of GalR in the hippocampus. Thus, pilocarpine-induced SE led to a 30% downregulation of GalR2 without affecting GalR1 (personal communication with T. Bartfai, Scripps Research Institute). Therefore, despite the fact that GalR2 co
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In the present study we also found
2021-10-28

In the present study, we also found that specificity concerns persist for antibody-based tools, like ELISAs. Measuring the same human plasma sample with four different commercial galanin ELISA kits produced four widely different galanin concentrations. No recovery of synthetic galanin peptide added
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Mitochondria are also involved in other modalities of progra
2021-10-28

Mitochondria are also involved in other modalities of programmed cell death, particularly apoptosis. Intriguingly, the roles of mitochondria in apoptosis and ferroptosis are fundamentally different. In mitochondria-mediated apoptosis, the mitochondrion serves as a reservoir, storing apoptosis-regul
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To validate that our natural experiment operates primarily
2021-10-28

To validate that our natural experiment operates primarily through a large negative shock to the risk-taking incentives provided by option compensation measured by vega, we do two sets of tests. First, we confirm a significant drop in vega after the adoption of FAS 123R for treated firms relative to
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Integrase inhibitors have been licensed for use in the UK
2021-10-28

Integrase inhibitors have been licensed for use in the UK since 2008. BHIVA now recommend starting all treatment naïve patients on a regimen containing two NRTIs, plus one of the following: a ritonavir boosted PI, an NNRTI, or an integrase inhibitor. They make further recommendations for patients wi
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