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br Conclusions This study showed that in EOC cells tyrosine
2020-10-23
Conclusions This study showed that in EOC cells, tyrosine kinase receptor DDR1 was expressed mainly in EOC SB 415286 with an Epithelial phenotype. The repressed expression of DDR1 in EOC cells with Mesenchymal phenotype could be due to the higher CpG methylation levels observed at the promoter o
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The IP R is a ubiquitously expressed Ca release channel
2020-10-23
The IP3R is a ubiquitously expressed Ca2+-release channel from the ER, activated by IP3, produced upon cellular stimulation by hormones, growth factors or neurotransmitters. Three genes are coding for the IP3R and their gene products (IP3R1, IP3R2, IP3R3) assemble in functional homo- or heterotetram
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Compounds and administered orally to fasted Harlan
2020-10-23
Compounds , , and administered orally to fasted Harlan Sprague-Dawley rats 1h prior to trigeminal stimulation, decreased extravasation in this model in a dose-related manner, with an estimated ID of 1, 10 and 100μg/kg, respectively (determined 15min after stimulation, ). For comparison, the clinical
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br Results br Discussion Drug
2020-10-23
Results Discussion Drug resistance poses the greatest hurdle of achieving high efficacy with AADs in cancer patients. AAD-treated cancer patients often encounter intrinsic and evasive drug resistance that diminishes the therapeutic efficacy to only minor survival benefits in most cancer types.
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Gamboge is a dry resin obtained from
2020-10-23
Gamboge is a dry resin obtained from Garcinia hanburyi HOOK. f. (Guttiferae). It has a variety of bioactivities, including detoxifying, homeostasis maintaining, anti-inflammatory and parasiticidic effects. Available evidence suggests that gamboge bears anticancer characteristics with gambogenic Taur
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First we synthesized inhibitor following the patent procedur
2020-10-23
First, we synthesized inhibitor following the patent procedure reported by Shewchuk et al. to provide its first complete characterization (see ). Two different synthetic approaches were used to obtain compounds –. The first method relied on the alkylation of the common 5-phenol-2,4-diaminopyrimidine
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We have previously characterized the leucine rich NESs
2020-10-23
We have previously characterized the leucine-rich NESs located within the zinc-binding domains of mucosal high risk HPV16 E7 (76IRTLEDLLM84) and low risk HPV11 E7 (76IRQLQDLLL84) mediating their nuclear export in a CRM1 dependent manner (Knapp et al., 2009, McKee et al., 2013). The zinc-binding doma
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Our study demonstrated that the sequential events of PKA
2020-10-23
Our study demonstrated that the sequential events of PKA and AMPK activation were involved in kinsenoside-mediated lipolysis. Within 1 h, PKA transiently inhibited AMPK activation by mitigating LKB1-mediated AMPK phosphorylation at Thr172, and PKA reduced AMPK-mediated phosphorylation at HSL-Ser565
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In previous works Gotor Vila
2020-10-23
In previous works (Gotor-Vila et al., 2017c), differences in solubility between the two carriers used during formulation were evidenced. Summarizing, maltodextrin (BA3 product) resulted in a much more soluble product since this polysaccharide is typically composed of an amount of reducing sugars bet
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br Coactivator Binding Sets APC C Catalytic Core
2020-10-23
Coactivator Binding Sets APC/C Catalytic Core in Motion A coactivator not only recruits substrates to APC/C [18] (Figure 3B), but also stimulates repositioning of the catalytic core 19, 24. High-resolution cryo-EM maps of apo forms of APC/C without a coactivator show the catalytic core and platfo
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In this study we implicate SCFFBXO E
2020-10-23
In this study, we implicate SCFFBXO3 E3 ligase as a critical modulator of inflammation in atherosclerosis and demonstrate the efficacy of a small molecule FBXO3 inhibitor in suppressing inflammatory responses important in atherosclerosis. Specifically, individuals carrying a hypofunctioning genetic
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From an industrial perspective the low turnover numbers
2020-10-22
From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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Introduction Glucose is the major carbon source in
2020-10-22
Introduction Glucose is the major carbon source in most organisms. Cancer bapta am in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammals is mainly media
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JNJ-54781532 Furthermore elastase might not be the only
2020-10-22
Furthermore, elastase might not be the only regulator of CBG on cleaved and uncleaved form. In a study by Nenke et al. [85] α1-AT deficient subjects, who lack this native neutrophil elastase inhibitor, paradoxically have higher levels of uncleaved CBG and lower levels of CBG* [85]. Gender differenc
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Introduction Collagen fibrillogenesis the assembly of collag
2020-10-22
Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the integrity of the whole tissue. Even a single point
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