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br Materials and methods br Acknowledgments We are grateful
2021-12-13

Materials and methods Acknowledgments We are grateful for financial support from the National Natural Science Foundation of China (Grants No. 81661148046 and 81773762, China) and the “Personalized Medicines—Molecular Signature-based Drug Discovery and Development”, Strategic Priority Research
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To investigate an involvement of
2021-12-13

To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) Lenalidomide were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-63 cells, while
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In this study according to the critical
2021-12-13

In this study, according to the critical pharmacophore T31, Y113 and R140 of FBPase, using the strategy of pharmacophore-based virtual screening, a series of novel scaffold inhibitor targeted the AMP binding site of FBPase were screened, their inhibitory activities against FBPase were further tested
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In the Medicines for Malaria Venture MMV distributed the Ope
2021-12-13

In 2011 the Medicines for Malaria Venture (MMV) distributed the Open-Access Malaria Box to accelerate antimalarial drug discovery (Spangenberg et al., 2013). The Malaria Box consists of 400 structurally diverse compounds, curated from >20,000 hits generated from large-scale screens, that inhibit the
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Fmoc-His(Trt)-OH Macrocycle was synthesized as described in
2021-12-13

Macrocycle was synthesized as described in , . Under SAr conditions, 2-chloronicotinonitrile was heated with -butyl 5-aminopentanoate in refluxing ethanol (). The resulting aminopyridine was treated with mesyl chloride and the nitrile was subsequently reduced to afford amine . Chloroaminopyrimidine
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Enhancer of zeste homolog EZH which functions as a
2021-12-13

Enhancer of zeste homolog 2 (EZH2), which functions as a methyltransferase, is a critical subunit of polycomb repressive complex 2 (PRC2), which has been demonstrated to be involved in the development of the Cy3 maleimide (non-sulfonated) [23]. Aberrant expression of EZH2 has been found to be assoc
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The root of Danshen has been widely used as
2021-12-13

The root of (Danshen) has been widely used as traditional Chinese medicine for many years and shown to exhibit significant pharmacological activities for a variety of human diseases including cancers. Tanshinones, the major active components, belong to a group of an abietane-type diterpenes contain
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When studying the potential of HATi for the treatment of
2021-12-13

When studying the potential of HATi for the treatment of inflammatory lung diseases, investigating lung tissue specific effects may be particularly relevant since local administration of small molecule inhibitors in lung tissue is possible and is already applied for inhaled glucocorticoids in the tr
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Here we examine the impact of hypoxia on lake whitefish
2021-12-10

Here we examine the impact of hypoxia on lake whitefish (Coregonus clupeaformis) during embryonic and larval development. Lake whitefish are a cold-water salmonid endemic to North America and are found from western Alaska, USA to eastern Labrador in Canada. Spawning occurs from late autumn to early
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Intestinal epithelium renewal is tightly controlled by Hedge
2021-12-10

Intestinal epithelium renewal is tightly controlled by Hedgehog genes. Three Hedgehog genes are highly conserved in mouse and human, including Sonic hedgehog (Shh), Indian hedgehog (Ihh), and Desert hedgehog (Dhh) [13]. Hedgehogs bind to Patched (PTCH) [[14], [15], [16]], which unlike conventional r
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Mathematical models play an important role in understanding
2021-12-10

Mathematical models play an important role in understanding and predicting the dynamic process of HBV infection. In the 1990s, Nowak et al. proposed a basic model to analyze the effect of antiviral treatment on reducing viral loads (Nowak et al., 1996). Since then, many different mathematical models
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Functional studies based on patch clamp electrophysiology pr
2021-12-10

Functional studies based on patch-clamp electrophysiology provide additional information on the active state of GlyR α1. Current-voltage measurements from single substance p in outside-out patches at symmetric 145-mM chloride concentration yielded a unitary conductance of 86 pS for the main open st
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NKH 477 The LBD experiences a large scale
2021-12-10

The LBD experiences a large-scale conformational transition between open and closed states upon agonist binding within the cleft separating the two lobes of the domain. The upper lobe (Lobe 1, also called D1) is connected to the ATD, and the lower lobe (Lobe 2, also called D2) is connected to the TM
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In conclusion enhanced glucagon action of the beta
2021-12-10

In conclusion, enhanced glucagon action of the beta cell results in improved beta cell function after glucose stimulation, but simultaneously dissociated responses to both glucose-dependent and non-glucose secretagogues evolve. This shows that the glucagon receptor is complexly involved in beta cell
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egfr inhibitor Cellular inhibition is caused by the hyperpol
2021-12-10

Cellular inhibition is caused by the hyperpolarization of the cell and is mediated by both synaptic and extrasynaptic GABAARs. Synaptic GABAARs are sensitive to high concentrations of GABA released at the synapse and mediate phasic inhibition. In contrast, extrasynaptic GABAARs mediate tonic inhibit
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