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br Author contribution br Acknowledgements QNRF grant
2020-09-15

Author contribution Acknowledgements QNRF grant number NPRP6-065-3-012, Qatar National Research Fund, Doha Qatar for funding this work with grant number NPRP No.: NPRP6-065-3-012. Introduction Preeclampsia (PE) affects 3–5 % of pregnancies worldwide and is one of the leading causes of mate
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TNF-alpha, recombinant human protein This work is inspired b
2020-09-15

This work is inspired by the systematic work of Coutinho and co-workers, who obtained several very useful experimental data, which will be also used in our work, and applied the CPA equation of state for the modeling of systems relevant to the production of biodiesel [8], [9], [10], [11], [12], [13]
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This structure guided the variation
2020-09-15

This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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This structure guided the variation
2020-09-15

This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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We observed the IVM potentiation of currents induced by
2020-09-15

We observed the IVM potentiation of currents induced by the EC5 of Glu or GABA and the IVM inhibition of currents induced by the EC90 of Glu or GABA in wild-type GluCls and GABACls. The EC50 of IVM for the potentiation in GluCls was 3.5-fold smaller than that in GABACls (Fig. 4, Fig. 8B, Table 2), a
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Evidence for interactions between the endothelin and the ang
2020-09-15

Evidence for interactions between the endothelin and the angiotensin system has also become plentiful. It has become clear that the two systems, in addition to acting independently, can act synergistically (Emori et al., 1989, Imai et al., 1992) as well as promote the peptide mRNA expression in endo
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N Cyclopentylmethyl analog exhibited fold less potent
2020-09-15

N-Cyclopentylmethyl analog 25 exhibited 2.3-fold less potent receptor affinity and 1.6-fold less potent antagonist activity. Among the compounds tested, the N-isobutyl analog 23 showed the most potent EP1 receptor affinity and antagonist activity. In summary, a series of 4-( 2-[alkyl(phenylsulfonyl
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Gupta et al have shown that a genetic
2020-09-15

Gupta et al have shown that a genetic variant associated with the 5 vascular diseases (coronary artery disease, migraine, carotid artery dissection, fibro-muscular dysplasia, and hypertension) is a distal regulator of the ET-1 gene [30]. They found that a single nucleotide polymorphism (SNP) locate
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br Funding br Disclosure of
2020-09-15

Funding Disclosure of interest Acknowledgments Introduction Pulmonary fibrosis (PF) is a chronic disease characterized by extensive deposits of the extracellular matrix (ECM) that can impair the architecture and function of the lungs (Cavazza et al., 2010). Imbalance between the prolifer
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The generation of ROS in
2020-09-14

The generation of ROS, in addition to eliciting oxidative stress, is an important proapoptotic signal (Ott et al., 2007). Apoptosis is clearly associated with the production of ROS, since ROS generation occurs in the mitochondrial respiratory chain and disturbs mitochondrial homeostasis, which plays
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Studies have focused on a hydrophobic
2020-09-14

Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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br Conclusion br Introduction br CRL E
2020-09-14

Conclusion Introduction CRL4 E3 ligases in tumorigenesis Small molecule-based PROTACs PROTAC: Major biological impacts Acknowledgements The authors sincerely apologize to all those colleagues whose important work was not cited in this paper owing to space limitations. They thank th
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In this study we implicate SCFFBXO E ligase as a
2020-09-14

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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832 582 4016 Real time PCR as described previously with mino
2020-09-14

Real-time PCR, as described previously with minor modifications, was used to detect DNA . The PCR mixture (Qiagen) was as follows: 5mM MgCl2, 2.5μl of 10x PCR Buffer, 0.125μl of HotStarTaq DNA Polymerase, 0.25mM of each dNTP, 0.4μM of each primer and 0.1μM of FAMlabelled probe (‘5-aacaattggagggcaag
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High throughput screening HTS of the AstraZeneca compound co
2020-09-14

High throughput screening (HTS) of the AstraZeneca Cinacalcet collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and wa
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