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Indeed the alkyl group is not seen in the original
2020-11-11
Indeed, the -alkyl group is not seen in the original crystallographic electron density omit map prior to positioning either inhibitor in DHODH, nor can it be found in the final maps. Rather, the electron density maps are consistent with hydrolysis of the amide to the acid. Once the scaffold was clea
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We recently reported that the
2020-11-11
We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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The use of SP in IPTp may not
2020-11-11
The use of SP in IPTp may not be the only driver of parasite polymorphisms in this population, because Senegal has used sulfadoxine and/or pyrimethamine in the national antimalarial treatment plan for many years, and furthermore these drugs are still being used in antibacterial combination therapy.
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ODQ mg br Molecular modeling simulation study
2020-11-11
Molecular modeling simulation study Molecular modeling study was performed through docking of the test compounds into the binding site of hDHFR enzyme using Discovery Studio 2.5 software. Computational docking is an algorithm designed to determine the suitable position and the orientation of the
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Preparation of the regioisomeric pyridooxazepinones and was
2020-11-11
Preparation of the regioisomeric pyridooxazepinones 10 and 11 was accomplished utilizing the synthetic sequence depicted in Scheme 3. Amide coupling of 63 and ZD 7288 chloride 64 afforded amide 65. Removal of the alcohol protecting group, followed by base catalyzed cyclization afforded a 1:2.4 mixt
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While these previous correlative studies have measured
2020-11-11
While these previous correlative studies have measured tDDR1 protein by IHC, these studies have not considered that pDDR1 could also be an important marker of cancer prognosis. A phosphoproteomic survey of lung cancer tissues did identify pDDR1 as one of the most commonly phosphorylated receptor kin
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Colony stimulating factor receptor CSF R or
2020-11-11
Colony stimulating factor-1 receptor (CSF-1R or cFMS) is a type III receptor tyrosine kinase. It is activated by binding with CSF-1 and IL-34, which stimulates differentiation, proliferation, survival and migration of monocyte-macrophage lineage cells., , , Also, macrophages produce inflammatory med
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br Functional significance Defects of the lysyl hydroxylases
2020-11-11
Functional significance Defects of the lysyl hydroxylases LH1, LH2, and LH3 impair collagen secretion and stability in the extracellular matrix, and cause rare connective tissue disorders such as Ehlers-Danlos type-VI [27], Bruck syndrome [28], and skeletal dysplasia [29], respectively. Elucidati
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br Loss of Chk sensitizes cells to hypoxia
2020-11-11
Loss of Chk 1 sensitizes BMS265246 mg to hypoxia/reoxygenation In contrast to Chk 2, studies have identified Chk 1 as being phosphorylated in an ATR-dependent manner at residue serine 345 during hypoxia [18]. More recently, siRNA mediated inhibition of Chk 1 signaling was found to sensitize cell
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Nociceptive and hyperalgesic actions of ET
2020-11-11
Nociceptive and hyperalgesic actions of ET-1 are produced through ETA and ETB receptors. Previous reports indicate that ETA receptor antagonists in peripheral tissues are effective in inhibiting ET-1 induced hyperalgesia, and attenuation of neuropathic pain in rats [16]. Studies have also shown that
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Several large scale clinical studies have
2020-11-11
Several large-scale clinical studies have set out with the common goal to further understand the cognitive impact of menopause and hormone therapies taken by women (Gleason et al., 2015, Greendale et al., 2011, Karlamangla et al., 2017, Rapp et al., 2003, Shumaker et al., 2003). Only one human study
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br Conflicts of interest br Acknowledgements This
2020-11-10
Conflicts of interest Acknowledgements This work was supported, in part or in whole, by the grants from the National Natural Science Foundation of China (11802056, 11772088), the China Postdoctoral Science Foundation (2018M640904), and the Fundamental Research Funds for the Central Universitie
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EC barrier dysfunction triggered by inflammatory mediators
2020-11-10
EC barrier dysfunction triggered by inflammatory mediators involves more than one mechanism, explaining the partial attenuation of EC barrier compromise obtained with PKA and Epac activators. PKA-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) has been shown to make a posit
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Conventional aromatic radiofluorination via nucleophilic sub
2020-11-10
Conventional aromatic radiofluorination via nucleophilic substitution requires electron-withdrawing activating group(s) at the ortho or para position to achieve good radiolabeling yield. In the case of CJ-042794 (), the phenoxy substitution para to the fluoro group is considered an electro-donating
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br Acknowledgements br Introduction Endothelial cells consti
2020-11-10
Acknowledgements Introduction Endothelial figure 1 constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile roles in mai
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