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CB-5083 synthesis To develop novel EPAC inhibitors
2020-08-22
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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A growing body of data indicates that
2020-08-21
A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream Fomepizole mg molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a reduction in the concent
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Our results showed that in elastase induced AAA
2020-08-21
Our results showed that in elastase-induced AAA, TGF-β neutralization finely tunes macrophage phenotype. Note that several studies have already addressed the role of M1 markers, such as IL-6 and IL-1β, or M2 markers, including IL-10 and TGF-β.4, 9, 10, 11 The expression and the role of ARG1 in AAA h
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br Compliance with ethical standards
2020-08-21
Compliance with ethical standards This work was conducted in compliance with ethical standards. Conflict of interest Funding The work was funded by extra mural research grant (EMR/2016/005135) from Science and Engineering Research Board, Government of India. Acknowledgements Introduc
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br Experimental Procedures br Acknowledgments The
2020-08-21
Experimental Procedures Acknowledgments The authors wish to thank P. Costet (University of Bordeaux) and Véronique Guyonnet-Duperat (FR TransBioMed, Plateforme de Vectorologie, University of Bordeaux) and Prof. Nils-Göran Larsson and Dr. Bettina Bertalan (Max Planck Institute for Biology of Ag
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Air trapping at the small airways is related to
2020-08-21
Air-trapping at the small airways is related to severe Kif15-IN-2 (Bjermer, 2014), and acute exacerbation (Mahut et al., 2010). Although asthma patients are generally treated with inhaled corticosteroid (ICS) or with ICS and long-acting β2 agonist (LABA), the efficacy of such treatment depends on d
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AMD is equally active against
2020-08-21
AMD3100 is equally active against a broad range of HIV-1 and HIV-2 strains, but not against simian immunodeficiency virus (SIV) strains in human PBMC (De Clercq et al., 1994). At this moment it is not clear what coreceptor SIV is using in human PBMC, but it does not seem to be CXCR-4 (Feng et al., 1
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Application of the CPH model
2020-08-21
Application of the CPH model relies on the assumption that the hazard ratio of two observations is constant over time [2]. This enables us to infer the rate of risk of the treatment. For example, in the study of patients with pulmonary arterial hypertension (PAH) [5], the hazard ratio of a group of
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While lowering the TID exposure
2020-08-21
While lowering the TID exposure of electronics is fairly straightforward, there are other Brilliant Blue G induced effects that are not as easily mitigated, especially with COTS components. Single Event Effects (SEE) occur when a high-energy particle strikes the active area of an integrated circuit
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Co operation or synergy between PKA and Epac
2020-08-21
Co-operation or synergy between PKA and Epac has been recently reported in PCCL3 thyroid cell line in which cAMP is pro-mitogenic, in Iodoacetyl-LC-Biotin to VSMC [19]. Our study demonstrates for the first time that PKA and Epac also synergise to inhibit cell proliferation in a cell type where cAMP
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br Authors contribution br Disclosure statement br Acknowled
2020-08-20
Authors contribution Disclosure statement Acknowledgements This study has received funding from the Italian Ministry of University and Research (PRIN 2015, grant number 2015373Z39_008) and from the Innovative Medicines Initiative 2 Joint Undertaking under grant agreement No 115797 (INNODIA)
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In this study EDC NHS crosslinked collagen films were deriva
2020-08-20
In this study, EDC/NHS crosslinked collagen films were derivatised with VWFIIINle-containing THPs and the effect on VWF and DDR2 activity was examined. First, we investigated restoration of the binding of DDR2 and VWF A3. Cell behavior beyond simple binding was also investigated through DDR2 Mirtaz
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br Materials and methods br Results br Discussion Our study
2020-08-20
Materials and methods Results Discussion Our study assessed the cytokine and chemokine changes associated with first onset PP as compared to HP and HNP groups. In the monocytes/ macrophages/ dendritic Bindarit synthesis panel, IL-6 levels were found to be significantly elevated in both HP
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br Discussion In depression an activation of the inflammatio
2020-08-20
Discussion In depression, an activation of the inflammation process and production of cytokines (including chemotactic cytokines – chemokines) and their receptors may occur due to the stimulation of the immune system. One of the earliest studied and described cytokines in depression is interleuki
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Although many GPCR heteromers have been
2020-08-19
Although many GPCR heteromers have been identified using heterologous cell lines, only very few fit all three criteria. This is mainly due to the difficulties to study these structures in native tissues because of the lack of sensitive and selective tools, not only capable of detecting in vivo evide
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