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ApicomplexansApicomplexans are unicellular and spore forming
2020-03-11

ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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Conventional aromatic radiofluorination via nucleophilic sub
2020-03-11

Conventional aromatic radiofluorination via nucleophilic substitution requires electron-withdrawing activating group(s) at the ortho or para position to achieve good radiolabeling yield. In the case of CJ-042794 (), the phenoxy substitution para to the fluoro group is considered an electro-donating
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Upon Edn ligand binding endothelin receptors can induce a va
2020-03-11

Upon Edn ligand binding, endothelin receptors can induce a variety of intracellular signaling cascades leading to diverse cellular responses such as contraction in the case of smooth muscle cells, or cell growth and mitogenesis. Ednrs are expressed in a variety of cell types and tissues, for example
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br Effects of culture conditions on drug
2020-03-10

Effects of culture conditions on drug-induced gene Valproic acid synthesis in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment that ar
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Nimodipine is an L type calcium channel antagonist that redu
2020-03-10

Nimodipine is an L-type calcium channel antagonist that reduces excessive calcium influx during pathological conditions, contributing to its neuroprotective properties (Zornow and Prough, 1996; Kobayashi and Mori, 1998). Autophagy can be induced by increased [Ca2+] (Rami et al., 2008). Nimodipine si
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E ligases provide substrate recognition specificity Ubiquiti
2020-03-10

E3 ligases provide substrate recognition specificity Ubiquitination tcid mg and substrate specificity in mammals is achieved by the existence of over six-hundred E3-ubiquitin ligases that catalyze the final step of ubiquitination, compared with only one E1 and very few E2 enzymes known till date [2
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Some mechanistic experiments performed in the early s by
2020-03-10

Some mechanistic experiments performed in the early 2000s by Ongusaha et al. [78], suggest that DDR1 induction protects Cholesterol from apoptosis in a p53-dependent manner, and that impairment of DDR1 expression or function leads to a pronounced increase of DNA damage-induced apoptosis. This eviden
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In this study cell migration in
2020-03-10

In this study, cell migration in response to LTD4 exhibited a typical bell-shaped dose-response curve with optimal activity at 10 nM. However, the effect of inhaled CysLTs on airway inflammatory cells in vivo has not been widely reported to date, therefore, the role of CysLTs in the development of a
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Therefore evaluation of base substances of alkali activated
2020-03-10

Therefore, evaluation of LY 2389575 hydrochloride substances of alkali-activated paste and alkali solution dosages have a remarkable impact on output products. Few research can be found in literature to assess GGBFS as a base materials of AAC. Even though less studies exists for serving RHA as base
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Here we explored the relative
2020-03-10

Here we explored the relative contribution of D1-like and D2-like receptor subtypes in the control of glutamate release, as well as their pharmacological properties and their interactions modulating the release. The pharmacological parameters (EC50 and Emax) of dopamine for the different types of re
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The inhibition of DNMT using AZA dC or DNMT
2020-03-10

The inhibition of DNMT1 using 5-AZA-dC or DNMT1 siRNA increased TIMP2 protein and mRNA expression, suggesting that TIMP2 expression is down-regulated by DNA methylation in the HDFs. In addition, 5-AZA-dC treatment led to a dose-dependent decrease of DNMT1 protein expression. 5-AZA-dC is a cytosine a
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The identification of a gatekeeper
2020-03-10

The identification of a gatekeeper L-365,260 also suggests that alternative DDR2 inhibitors may be required to overcome acquired resistance. Additional DDR2 inhibitors that have been isolated include the recently identified alkaloid natural products discoipyrroles A-D and the chemotherapeutic Actin
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br Signaling of DDR receptor and its
2020-03-10

Signaling of DDR2 receptor and its regulation Being the tyrosine kinase receptor, downstream signaling of DDR2 receptor is initiated by phosphorylation of cytoplasmic tyrosine residue upon ligand binding (Type II collagen) but the authentic facts or detail information of tyrosine phosphorylation
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Several reports by us and others have highlighted
2020-03-10

Several reports by us and others have highlighted that dimerization or oligomerization of DDR1 ECD and DDR2 ECD enhances their binding to triple-helical collagen.18, 19, 22, 28, 29, 30, 31 The ECD of DDRs consists of a discoidin domain and a stalk region. It has been reported that independent Nafamo
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Desformylflustrabromine hydrochloride synthesis We have prev
2020-03-10

We have previously reported DAPK inhibitors discovered through our structure-based virtual screening (SBVS) research program. In this paper, we describe the general protocol of our in silico approach, and the strategy used to develop hit compounds. In addition, the studies conducted on the structure
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