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Several effective strategies have been
2021-03-23

Several effective strategies have been developed to design activatable MR probes according to the Solomon, Bloembergen and Morgan (SBM) theory, including modulation of the number of inner-sphere water molecules (q), the rotational tumbling time (τ) and the residence lifetime of inner-sphere water mo
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Potential break through technology poised to overcome these
2021-03-23

Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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A growing body of data indicates that
2021-03-23

A growing body of data indicates that endothelial NOS (eNOS) is a rate-limiting enzyme for the synthesis of nitric oxide (NO), its downstream 7α,25-dihydroxy Cholesterol receptor molecule. High pathological concentrations of NO produced from inducible NO synthase (iNOS) induce apoptosis, whereas a
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In general cellular senescence is
2021-03-23

In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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Two parameters were extracted from these experiments to comp
2021-03-23

Two parameters were extracted from these experiments to compare the interactions of the three compounds with ct-DNA. The association constant K for the binding of the naphthalimide derivatives to ct-DNA was calculated by fitting the evolution of the fluorescence spectra with a 1:1 binding model usin
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price scd The TELI results of DNA damage responses to CAA
2021-03-23

The TELI results of DNA damage responses to CAA and SO then informed our choice of bacterial strains in subsequent experiments. We investigated E. coli cellular survival in response to CAA and SO exposure by determining the sensitivity of a number of E. coli strains, each possessing single or multip
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A novel series of DHODH inhibitors was developed by
2021-03-23

A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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Regarding the mechanism of action of CRF several studies
2021-03-22

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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To understand the behavior of enzymes in ILs
2021-03-22

To understand the behavior of enzymes in ILs at a molecular level, it is first desirable to dissolve enzymes in the solvents. For soluble catalysts, there are many relatively simple spectroscopic and other techniques for obtaining accurate information at a molecular level. Parker et al. [9] reported
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Multiple protein species are known to naturally exist
2021-03-22

Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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In vitro studies in NSCLC cell lines
2021-03-22

In vitro studies in NSCLC cell lines expressing EGFR mutants (T790M mutation, exon 19 deletion E746-A750, L858R/T790M double mutation), demonstrated that Rociletinib potently inhibits proliferation in the mutant EGFR NSCLC CCT007093 with Growth inhibition (GI50) values ranging from 7 to 32 nmol/L.
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Ingested folate needs to be chemically modified in order to
2021-03-22

Ingested folate needs to be chemically modified in order to become a one carbon donor for cell metabolism. Firstly, folate turns to dihydrofolic dub inhibitor (DHF), it is then converted into tetrahydrofolate (THF) by the dihydrofolate reductase enzyme (DHFR) and finally converted into N5, N10-meth
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br Role of ALDH Isoenzymes in
2021-03-22

Role of ALDH Isoenzymes in Glioma Growth and Invasion ALDH family genes are commonly upregulated in gliomas, indicating ALDH-dependent cell metabolism. Specific ALDH isoenzymes have been detected in high- and low-grade tumors implicated in cell proliferation, maintenance of CSC properties, invasi
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ApicomplexansApicomplexans are unicellular and spore forming
2021-03-22

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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SP 600125 Recently it was reported that Crm is
2021-03-22

Recently, it was reported that Crm1 is linked to spindle pole body (SPB) by Spc72 in SP 600125 yeast [9]. Spc72 and Spc110 are two specific receptors of γ-tubulin complex (Tub4), which target Tub4 to SPB and mediate the nucleation of microtubules from SPB [20]. It was found that disrupting the inter
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