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Our previous high throughput screening HTS campaign using
2021-01-05

Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based 69 8 australia assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22]
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br Conflict of interest statement br References
2021-01-05

Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We acknowledge financial support by the Swiss State Secretariat for Education, Research and Innovation (Federal
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Introduction The annual global market of industrial enzymes
2021-01-04

Introduction The annual global market of industrial 5-Methyl-UTP is reported to be billions of USD [1], [2], [3], [4], [5], [6], [7], and impacts commercial sectors that include energy, animal feed, household products, food processing and pharmaceuticals [1], [2], [5], [6]. Enzymatic processing is
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br Materials and methods br
2021-01-04

Materials and methods Results Discussion In addition, the responses of CYP450s induced by metalaxyl are species-specific in the four cells. For example, metalaxyl lead to induction of CYP1A1, CYP1A2, and CYP2B1 in HepG2 cells, CYP1A2 and CYP2B1 in H4IIE cells, CYP1A1 and CYP2B1 in LMH cells
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In this report we present spectroscopic evidence on
2021-01-04

In this report, we present spectroscopic evidence on the effect of different solvents having proton acceptor and proton donor ability and pH of the medium on the abstraction of amino proton of PI (Scheme 1) for controlling the nonradiative rates. Despite the general utility of PI as a DNA intercalat
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xec sale br Introduction In addition to the canonical double
2021-01-04

Introduction In addition to the canonical double stranded structure, DNA can form various higher order structures such as bulges, and various kinds of mismatches, triplexes, to the G-quadruplex (G4). Over the past decades, accumulating evidence has begun to emerge that these non-canonical structu
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Given the excellent in vitro pharmacology profiles of
2021-01-04

Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic neurokinin receptor functionality of 1. Acetonitrile 49 was found to have a good balance of
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br Endothelial mechanotransduction br Apoptosis
2021-01-04

Endothelial mechanotransduction Apoptosis Death associated protein kinase Conclusion DAPK is localized to the Neostigmine Bromide network, and promotes actomyosin contractility. DAPK stabilizes stress fibers by phosphorylation of MLC (Bialik et al., 2004, Kuo et al., 2003). In endotheli
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In frame exon skipping of COL A has been suspected
2021-01-04

In frame exon 41 skipping of COL6A3 has been suspected to be responsible for isolated dystonia in several human kindreds without muscular defects [94]. In order to validate their hypothesis, the authors used zebrafish to selectively knock down several exons in col6a3 and found a negative impact on m
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First of all two assumptions just as in Ref
2021-01-04

First of all, two assumptions just as in Ref. [30] are need to simplify the penetration process: (1) The crater phases is short and the p m x of EFP is consumed little; thus, the influence of crater on penetration can be ignored; (2) the initial stagnation radial pressure is equal to axial pressure,
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The assembly and maturation of invadopodia can be initiated
2021-01-04

The assembly and maturation of invadopodia can be initiated by chemical stimuli such as the epidermal growth factor (EGF), as well as the mechanical signals from extracellular matrix (ECM). Upon binding, EGF activates the EGF receptor (EGFR), which further activates several intracellular signaling p
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Previously we have described increased expression of both
2021-01-04

Previously, we have described increased expression of both cytokine and chemokine mRNA (e.g. MCP-5 and fractalkine) in the left ventricle of male EP4-KO mice with dilated cardiomyopathy [2]. Takayama et al. [31] have shown that PGE2 potently inhibits cytokine/chemokine secretion (MCP-1, interleukin
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Our finding that activating DDR variants
2021-01-04

Our finding that activating DDR2 variants are a cause of this disease suggested that the ABL inhibitor dasatinib, a leukemia drug that also inhibits DDR2, could be used for treatment of affected individuals.10, 11 To examine the effect of dasatinib on p.Leu610Pro- and p.Tyr740Cys-induced autophospho
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Previous in vitro and in vivo
2020-12-31

Previous in vitro and in vivo studies have shown the potent ability of toll-like receptor (TLR) ligands and type I interferon (IFN) signaling to induce CH25H in macrophages and DCs following exposure to innate immune stimuli (Bauman et al., 2009; Diczfalusy et al., 2009; Park and Scott, 2010; Zou et
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br Rationale Recently we have shown that the nasal CysLT
2020-12-31

Rationale Recently we have shown that the nasal CysLT2 receptor localized exclusively in blood vessels and the expression level of the CysLT2 receptor in patients with nasal allergy was higher than that in patients with non-allergic rhinitis (Shirasaki et al. Allergol Int 2013). We hypothesized t
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