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Tailoring pharmacological treatment to the genetic backgroun
2021-02-02

Tailoring pharmacological treatment to the genetic background of a person can enhance therapeutic response (), increase compliance (), and decrease drug toxicity (, , ). Because cocaine addiction has a strong genetic basis, with the vulnerability to develop an addiction estimated to be as high as 72
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Previous studies from our lab looked at the effect of
2021-02-02

Previous studies from our lab looked at the effect of interfering with crossover helix interactions in TS-DHFR. One study utilized peptide mimetics of the crossover helix to inhibit wild-type TS-DHFR noncompetitively, and with an IC of 230 μM. A second study used a virtual screening approach to ide
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For radiochemotherapy it is well known that mitotic cell dea
2021-02-02

For radiochemotherapy, it is well known that mitotic cell death and apoptosis present the major cell death modes. More recently, autophagy-dependent cell death has been described to occur upon radiochemotherapy (Daido et al., 2005, Song et al., 2017). This form of regulated cell death depends on com
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Interestingly some drugs have been
2021-02-02

Interestingly, some drugs have been shown to be effective in the regulation of cytokine production (such as IL-2, IL-10, IL-27, IL-35, IL-37 and transforming growth factor-β, TGF-β) and, therefore, having a key role in the management of certain inflammatory-based clinical conditions (Banchereau et a
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br Introduction Localized degenerative and
2021-02-02

Introduction Localized, degenerative and progressive enlargement of the aortic diameter involves all layers of the vessel wall may ultimately rupture creating a catastrophic cardiovascular event [1,2]. An aneurysm may be located in the thoracic or abdominal aortic wall with different clinical app
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The cyclin dependent kinase deactivation is carried out
2021-02-02

The cyclin-dependent kinase deactivation is carried out by a particular group of proteins cyclin-dependent kinase inhibitors (CDKIs). These group of proteins blocks kinase activity by interfering with the interaction of cyclin-CDK complex [43]. The inhibition of CDK naturally occurs during a G1 phas
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br Conclusion The preclinical data reported in this
2021-02-02

Conclusion The preclinical data reported in this study shows that LAS191859 is a potent and safe CRTh2 antagonist, with a long receptor residence time that provides a sustained in vivo efficacy. This property is reflected in the prolonged duration of action of LAS191859 in in vitro and in vivo fu
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The intricate roles and neural systems and
2021-02-02

The intricate roles and neural systems and mechanisms involved in the CRF1 and CRF2 mediation of spontaneous and stress-induced anxiety behavior remain to be defined. Of particular relevance are studies evaluating the behavioral actions of CRF1 and CRF2 receptors separately as well as together. For
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Finally naringin and hesperidin have
2021-02-02

Finally, naringin and hesperidin have different glycosidic moieties (neohesperidose α-1,2 and rutinose α-1,6 respectively), bound in the same C7 position on the A ring of the flavonoid. The higher value of k/KM of RHA-Phis towards the former substrate suggests that the enzyme shows a preferential hy
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In our former work our interest was in
2021-02-02

In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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To develop novel EPAC inhibitors Zhou and co
2021-02-02

To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dockin
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To understand the behavior of enzymes in ILs at a
2021-02-02

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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The main advantage of exploiting
2021-02-02

The main advantage of exploiting paper sludges as sources of cellulose-derived energy and chemicals in comparison to other lignocellulose substrates is their amenability, which is associated with an extensive pulping process that removes the majority of the lignin and exposes Sodium 4-Aminosalicylat
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br Methods br Results br Discussion Skin biopsy and microneu
2021-02-02

Methods Results Discussion Skin biopsy and microneurography have both been described as useful tools in the diagnosis of PAN, directly identifying peripheral sympathetic fibers without the mediation of specific Liproxstatin-1 organs (Donadio et al., 2005, Donadio et al., 2012a, Donadio and
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Six substrate recognition sites SRS SRS have been identified
2021-02-01

Six substrate recognition sites (SRS1-SRS6) have been identified at positions 102-123, 204-209, 238-244, 301-319, 374-382 and 483-492 (Table 2, underlined residues) based on Gotoh's proposal [30]. CYP3A163 displays the similar characteristic long sequences between helices F and G presenting two addi
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