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It would also be interesting to understand the potential con
2022-07-30

It would also be interesting to understand the potential connection between asymmetric histone inheritance and another phenomenon reported by several investigators: selective DNA strand segregation (reviewed by Evano and Tajbakhsh, 2013, Rando, 2007, Tajbakhsh and Gonzalez, 2009). Recent development
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Of xenobiotic quinones thymoquinone methyl isopropyl
2022-07-30

Of xenobiotic quinones, thymoquinone (2-methyl-5-isopropyl-1,4-benzoquinone; Fig. 1) is one of the most thoroughly studied for its pharmacological properties. It is the most active component of Nigella sativa, commonly called black cumin2, 3, the essential oil of the seeds of which are used for trea
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br For some time it was known that
2022-07-30

For some time, it was known that membrane-bound guanylate cyclases (GCs) of photoreceptor INK 128 in the retina respond to changes in the [Ca]. Lolley and Racz observed that synthesis of cyclic GMP (cGMP) was stimulated at only low [Ca], concluding that Ca has an inhibitory effect on the regulat
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Recent work by Que et al with mouse models
2022-07-30

Recent work by Que et al with mouse models implicates GSNOR in the cause of asthma. GSNOR is expressed in multiple cell types in the lung, including airway epithelial cells and infiltrating leukocytes. After exposure to ovalbumin, GSNOR activity increased in airway lining fluid, perhaps reflecting i
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br Introduction The generic antifibrinolytic drug tranexamic
2022-07-29

Introduction The generic antifibrinolytic drug tranexamic gap-26 (TXA) inhibits the protein-protein interaction between plasminogen and fibrin [9]. TXA is frequently used to reduce bleeding in various hemorrhagic conditions, such as during surgical procedures in the heart [19]. However, treatmen
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The ester moiety is a
2022-07-29

The ester moiety is a promising structural motif at the C-3 position for the development of drug-like molecules. However, the labile C-3 ester bond impels these derivate to be susceptible to plasmatic degradation by esterases and this is natural steroidal metabolic process [39,40]. Hence, the isoste
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The EEGs of these six patients interestingly
2022-07-29

The EEGs of these six patients interestingly showed focal, multi-focal and generalized spikes, which was an exclusion criteria in our study as we selected our cohort to exclusively represent focal epilepsy. Remarkably all of these cases were diagnosed with paroxysmal exercise-induced dyskinesia (PED
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br The actions of GLP on the vasculature endothelium
2022-07-29

The actions of GLP-1 (9–36) on the vasculature/endothelium The previous sections have ascribed the vascular and/or endothelial actions of GLP-1/GLP-1R agonists to potential direct actions through a canonical GLP-1R, but as mentioned previously, whether VSMCs and ECs express a full-length GLP-1R r
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The caseins are a family of
2022-07-29

The caseins are a family of milk phosphoproteins whose biological function is to provide supersaturating concentrations of calcium, phosphates, and essential Sodium 4-Aminosalicylate to the neonate (Vonderhaar and Ziska, 1989). α- and β-caseins, the most abundant of the milk caseins, are described
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We have previously designed an azobenzene based molecule Raz
2022-07-29

We have previously designed an azobenzene-based molecule, Razo, which could switch the conformations of G-quadruplex structures by photoregulation. 12, 13, 14, 15 However, it lacks selectivity to different G-quadruplexes. Therefore, we want to find a way to modify this molecule so that it could be u
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br Introduction Farnesoid X receptor FXR is a
2022-07-29

Introduction Farnesoid X receptor (FXR) is a bile CCCP regulated nuclear receptor highly expressed in the liver, intestine, kidney and adrenal glands in rodents.1, 2, 3, 4 FXR regulates transport proteins, the bile salt export pump (BSEP) and the organic solute transporter α (OSTα) that are invol
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Iloperidone receptor The highest metabolic stability observe
2022-07-29

The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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Lenvatinib is an orally available multi targeted tyrosine
2022-07-29

Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to
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FLAG tag Peptide GPR which is also known
2022-07-29

GPR40, which is also known as FFA receptor 1 (FFAR1 or FFA1), was identified as an orphan receptor in the search for novel human galanin receptor (GALR) subtypes in 1997. Using reverse pharmacology approaches measuring calcium transients, GPR40 were deorphanized and characterized as being activated
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br Results and discussion CATALYST software allows automatic
2022-07-29

Results and discussion CATALYST software allows automatic pharmacophore construction by using a collection of molecules with activities ranging over a number of orders of magnitude. In addition, CATALYST pharmacophores (hypotheses) explain the variability of bioactivity with respect to the geomet
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