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To simulate the inhibition of the enzyme by
2021-05-17
To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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Our earlier experimental studies showed neutral i e
2021-05-17
Our earlier experimental studies showed "neutral", i.e. non-proliferative, effects of progesterone but a large increase in proliferation using certain progestins; however, this was only in the presence of PGRMC1 [[13], [14], [15], [16], [17], [18], [19]]. The next step was to investigate whether thi
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Raloxifene is a second generation SERM that has tissue
2021-05-17
Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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Further modifications on the position
2021-05-17
Further modifications on the 8-position of compound led to compound 4 (8-pCPT-2′--Me-cAMP, a.k.a. 007, ), which is a potent (half-maximal activation of EPAC1 at 2.2µM) and selective (about 100-fold EPAC/PKA selectivity) EPAC agonist. Since the discovery of compound , it has been widely used as a po
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br Introduction The development of non melanoma skin cancer
2021-05-17
Introduction The development of non-melanoma skin cancer (NMSC) is a complex process characterized by the acquisition of altered proliferation and invasiveness. These changes are classically defined as occurring in stages, i.e., initiation, promotion, and progression. In the two-stage model of in
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In summary EP signaling modulates heteromeric kainate recept
2021-05-17
In summary, EP1 signaling modulates heteromeric kainate receptors at multiple steps, both sensitizing mice to kainate-evoked status epilepticus and, separately, exacerbating the downstream consequences of status epilepticus. These results, together with those of Serrano et al. (2011) and Jiang et al
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The Penicillium strain used in this
2021-05-17
The Penicillium strain used in this work was isolated from Atlantic forest soil and previously screened as lipase producer (Tauk-Tornisielo et al., 2005). The immobilization was previously evaluated using hydrophobic supports, i.e. agarose based butyl-(But), phenyl-(Phe) and octyl-Sepharose (Oct), a
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To study the effect of DDR
2021-05-17
To study the effect of DDR inhibition by imatinib, nilotinib and dasatinib in a cellular environment we generated DDR1 and DDR2 expressing HEK293 cell lines by stable transfection. Of the five DDR1 splice variants we focused on the 1b variant whose over-expression has been associated with pulmonary
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R115777 In conclusion we have shown that the cellular
2021-05-17
In conclusion, we have shown that the cellular effects produced by SFN in NSCLC R115777 are largely mediated by SFN-induced production of ROS. Cells with higher levels of EGFR were more resistant to SFN treatment and showed resistance to SFN-induced apoptosis, suggesting that high EGFR levels protec
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Our study found a significant association
2021-05-17
Our study found a significant association between the degree of primary tumor lobulation and EGFR mutations status (P EGFR Crotaline synthesis status. However, only a small portion of these previous studies included the evaluation of lobulation, and almost all of them reported no association betwee
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Mitomycin C How does APC C recognize its substrates and cata
2021-05-17
How does APC/C recognize its substrates and catalyze their ubiquitylation? How are the outcomes and timing of these activities regulated? These questions have driven a decade of structural studies that begin to explain how APC/C interacts with coactivators, substrates, and E2s, and how these interac
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In conclusion we have found that
2021-05-17
In conclusion, we have found that Egr1 can play an inhibitory role on DBH promoter-driven transcription. This inhibition requires a newly identified Egr1 response CGP41251 at the −227/−224 region of DBH promoter. This inhibition appears to result from Egr1 directly bound to the DBH promoter. We spe
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br Introduction Acinetobacter baumannii is a gram negative
2021-05-17
Introduction Acinetobacter baumannii is a gram-negative opportunistic pathogen that causes nosocomial infections including pneumonia and bloodstream infections which is associated with an increased mortality and multi-drug resistance [[1], [2], [3]]. A. baumannii was rated as one of the critical
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DNA methylation is associated with transcriptional silencing
2021-05-17
DNA methylation is associated with transcriptional silencing of tumor suppressors or other genes important for normal cellular function and plays an important role in the development of cancer and other diseases (such as breast and colorectal cancers) [19]. DNA methyltransferases (MTases) are a fami
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The second part of this study evaluated the
2021-05-14
The second part of this study evaluated the role of CK1 in the eFABP4 cellular uptake in endothelial cells. By blocking CK1 expression using a specific siRNA, we corroborated that the presence of CK1 was fundamental for FABP4 cellular uptake and internalization in endothelial cells, thus decreased m
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