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A high throughput screening campaign led to the discovery
2024-12-04
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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MADS box proteins are combinatorial
2024-12-04
MADS box proteins are combinatorial transcription factors in that they often derive their regulatory specificity from other DNA binding or accessory factors. In many cases, the cofactor with which MADS box proteins interact specifies which genes are regulated, when they are regulated and if these ge
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br LO synaptic integrity and memory Interestingly
2024-12-03
12/15LO, synaptic integrity, and memory Interestingly, several groups have found that 12/15LO directly modulates synaptic function. Normandin and colleagues reported that pharmacological inhibition of 12/15LO modulates rat hippocampal long-term depression (LTD), a process by which neuronal synapt
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br Materials and methods br
2024-12-03
Materials and methods Results Discussion The novel and central finding of the current study is that endothelial 12/15-LO rather than the monocytic/macrophagic 12/15-LO has a critical role in hyperglycemia-induced leukocyte adhesion and retinal endothelial barrier dysfunction. The following
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Naringin australia The mechanism of transformation into SCLC
2024-12-03
The mechanism of transformation into SCLC is unclear but the loss of retinoblastoma gene (RB) seems important and constitutes an initial event in the tumorigenic process. Some reports revealed the role of the RB gene loss in EGFR mutated NSCLC who transformed into SCLC [15]. In NGS we retrieved mut
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In a working group exposed
2024-12-03
In 2008, a working group exposed 12-month-old transgenic mice (mutation for human amyloid precursor protein expression) and their non-transgenic littermates to isoflurane and halothane for 120min per day for five days. It was concluded that in the transgenic mouse there was overload of amyloid prote
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The relatively high concentration of HT
2024-12-02
The relatively high concentration of 5-HT used in this study (100 µM) is consistent with the concentrations used in other published ex vivo studies (Ropert and Guy, 1991, Passani et al., 1994, Shen and Andrade, 1998). In our paradigm 5-HT was focally applied at the surface of the slice via a fast pe
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br Conflict s of interest br Retinopathy of prematurity
2024-12-02
Conflict(s) of interest Retinopathy of prematurity (ROP) is a leading cause of childhood blindness Retinopathy of prematurity (ROP) is a disease of premature infants which disrupts normal retinal vascularization (Fleck and McIntosh, 2008). With increased survival of extremely premature infants
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By applying each external load
2024-12-02
By applying each external load to the G-actin molecule, and measuring the elongation of the molecule, we computed force-displacement curves. The force versus displacement curve can be used to evaluate the tensile stiffness of the G-actin from a linear regression analysis. Followed by statistical ana
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Genetic observations from these studies suggest that
2024-12-02
Genetic observations from these studies suggest that GMF regulates Arp2/3 complex and chem 17 synthesis dynamics in vivo13, 14. Budding yeast Gmf1 localizes to cortical actin patches, sites of endocytosis assembled by Arp2/3 13, 14. Furthermore, deletion of GMF1 exacerbates the growth defects of a c
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rs G allele was previously associated with a decrease in
2024-12-02
rs523349 G allele was previously associated with a decrease in the conversion rate of testosterone to DHT (Beesley et al., 2007). This SRDA52 variant may have a trend towards higher testosterone availability, which according to the US Food and Drug Administration is described as a teratogen of categ
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Auranofin Despite functional studies demonstrating the role
2024-12-02
Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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Matrix metalloprotease inhibitors are increasingly available
2024-12-02
Matrix metalloprotease inhibitors are increasingly available and tested for other indications in clinical trials. The present study suggests that either ADAM10 or TACE inhibition alone will not maximally restore leukocyte Axl function. We found that lower doses of ADAM10/TACE inhibitors exhibit simi
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Nowadays more than kinases have
2024-12-02
Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme
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br Ataxia telangiectasia and Rad related as a therapeutic
2024-12-02
Ataxia–telangiectasia and Rad3 related as a therapeutic target Several concerns revolving around functional inhibition of ATR have hindered the exploitation of ATR as therapeutic target in cancer therapy and delayed the development of specific ATR kinase inhibitors. It was anticipated that pharma
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