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Exendin-4 br Results br Discussion Drug resistance poses the
2020-11-19
Results Discussion Drug resistance poses the greatest hurdle of achieving high efficacy with AADs in cancer patients. AAD-treated cancer patients often encounter intrinsic and evasive drug resistance that diminishes the therapeutic efficacy to only minor survival benefits in most cancer types.
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(+)-Catechin hydrate CK comprises a family of serine threoni
2020-11-19
CK1 comprises a family of serine/threonine protein kinases, that includes different CK1 isoforms namely α, β, δ, ε and γ their various splice variants [56]. It was reported that the pharmacological inhibitor IC261 shows an order of magnitude of higher selectivity for CK1δ or CK1ε isoforms (IC50 of 1
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br Conflict of interest br Acknowledgements This work was su
2020-11-19
Conflict of interest Acknowledgements This work was supported in part by JSPS KAKENHI Grant Number 26292031. We thank Nissan Chemical Industries, Ltd. for the gift of the sample of fluralaner. Introduction As one of the most common cancers in southern China and southeast Asia, nasopharynge
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Although several genomic technologies including the
2020-11-18
Although several genomic technologies, including the generation of ERRγ-specific knockout mice, have revealed that ERRγ plays a pivotal role in cellular bioenergetics [1], its involvement in other metabolic pathways has been appreciated only recently. Therefore, we highlight recent findings on the r
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Enzyme activity loss during the hydrolysis process has
2020-11-18
Enzyme activity loss during the hydrolysis process has traditionally been associated with thermal, mechanical, and/or chemical mechanisms (Okino et al., 2013, Ye et al., 2012, Zhang et al., 2010). Due to the recent discovery of enzyme activity loss due to interaction with substrate, it is important
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br Substoichiometric substrate modification E ligases
2020-11-18
Substoichiometric substrate modification E3 ligases catalyze the rapid transfer of the SUMOD from the E2 enzyme to the substrate. By definition, enzymes are recycled in the reaction, allowing multiple rounds of substrate modification by a single enzyme. Thus, enzymes function at substoichiometric
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br Materials and methods br Results
2020-11-18
Materials and methods Results In the leaves of the studied varieties, one to three nucleoli per nucleus were observed (Fig. 1a), except for the variety Bastardo were a maximum of two nucleoli per nucleus were detected. In the root-tip cells, most of the varieties presented one to three nucleo
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The biological significance of DNA ligases is attributed
2020-11-18
The biological significance of DNA ligases is attributed to their function in DNA replication, recombination and/or DNA repair [1], [2]. In vertebrates, three different DNA ligases I, III and IV are recognized. DNA ligase I is essential for the Okazaki fragments’ ligation during lagging-strand DNA s
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These reactions are used to account for
2020-11-18
These reactions are used to account for variations in protein solubility or vesicle recovery. For example, with DGKθ we have found it necessary to maintain the purified enzyme in a solution of 0.01% DDM (DGK-D dilution buffer) in the control reaction to prevent enzyme loss due to aggregation or adhe
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The overall poor outcomes in ESCC are
2020-11-17
The overall poor outcomes in ESCC are thought because of a combination of late diagnosis, aggressiveness of the disease, and a lack of effective treatment strategies for systemic disease. Several molecular pathways, such as epidermal growth factor receptor, vascular endothelial growth factor, and p5
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In a study on the
2020-11-17
In a study on the time course of a mechanism-based inactivation of CYP3A by HIV protease inhibitors, Katzenmaier et al. [37] reported that the suppression of CYP3A activity continued for threedays after the discontinuation of ritonavir. In the present study, the CYP3A activity on day 28 after a seve
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Considering the protumoral functions of TAMs
2020-11-17
Considering the protumoral functions of TAMs, new therapies against TAMs have recently gained interest. Such treatments, particularly inhibitors of the colony stimulating factor 1 receptor (CSF-1R), are currently evaluated in several clinical trials [19]. CSF-1R inhibitors may also be of interest in
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With the narrow SAR of the
2020-11-17
With the narrow SAR of the tail favouring the ortho sulfone group, we examined the remaining position open to substitution at the pyrazole 3-position, in an attempt to at least moderate the excessive human PPB (). Lipophilic groups in this position maintained huge shifts in potency in the absence or
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Several studies have described the
2020-11-17
Several studies have described the role of NP in vRNP nuclear export. For example, leptomycin B (LMB), an inhibitor of the CRM1 nuclear export signal (NES) binding domain (Kudo et al., 1999), inhibits nuclear export of vRNP and NP, but not NEP or M1, in virally infected or transfected cysteine prote
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Regarding the mechanism of action of CRF several studies
2020-11-17
Regarding the mechanism of action of CRF, several studies have shown that low doses of CRF may preferentially activate CRF1 receptors in glutamatergic projection neurons, serotoninergic neurons or glutamatergic collaterals in the medial prefrontal cortex (Vertes, 2004). Indeed, prosencephalic inacti
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