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br Halogenases Enzymatic C H activation leading to
2021-04-19
Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical
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With respect to the muscle compartment only low protein expr
2021-04-19
With respect to the muscle compartment, only low protein expression of ASB9 has been detected in healthy human skeletal muscle [as reported in the Human Protein Atlas (HPA)], whereas high levels of Asb5 protein expression are detected in mammalian skeletal muscle, which appears to be important in th
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Further indirect evidence supporting an important role
2021-04-19
Further indirect evidence supporting an important role of DPP-4 in the modulating the actions of both incretins comes from the observations that analogues of GLP-1 and GIP, modified to be resistant to DPP-4 cleavage, were subsequently shown to have greater metabolic stability in vivo which was assoc
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br Results br Discussion Many assays in the literature for
2021-04-19
Results Discussion Many assays in the literature for DBH require the use of catalase to protect the active site from hydrogen peroxide, which is a by-product in the initial step of the reaction. For the non-immobilized enzyme there was a visible increase in the rate with increasing amounts of
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br GPCRs form heterotetramers In addition to
2021-04-19
GPCRs form heterotetramers In addition to homodimers and heterodimers, for several family A receptor heteromers, experimental evidence supports the presence of higher order rearrangements as tetrameric structures, comprised of two different homodimers, each able to signal with its preferred G pro
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Tumor cells exposed to the effect of these compounds were
2021-04-19
Tumor 3965 synthesis exposed to the effect of these compounds were shown to become chemo and radio-sensitive. Based on that, it was possible to anticipate the selectivity requirement for DNA-PK inhibition and the best route for their development. Accordingly, prompted by the clinical significance a
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During germ cell development in
2021-04-19
During germ cell development in mouse, de novo Dnmts regulate the genomic imprinting and silence of repeat elements. Dnmt3A methylated H19, Dlk1/Gtl2, and Sine B1, whereas Dnmt3B methylated microsatellite repeat elements, the two Dnmts co-methylatedRasgrf1, IAP, and Line1 repeat elements (Lucifero e
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In addition to through direct regulation
2021-04-19
In addition to through direct regulation of cell differentiation, DDR2 may raise the abundance of myofibroblast subsets through advancing the recruitment of its precursor cells. One such evidence is that DDR2 can regulate lung fibroblast proliferation and migration. Another possibility rests on the
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Interestingly increased level of both circulating ET and
2021-04-17
Interestingly, increased level of both circulating ET-1 and urinary excretion of ET-1 have been observed in patients treated with nephrotoxic immunosuppressive agents as cyclosporine A and tacrolimus (Slowinski et al., 2002). Other nephrotoxic agents, such as cisplatin, also increase urinary excreti
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Together the data suggests that more work needs
2021-04-17
Together, the data suggests that more work needs to be done to establish the role of PARP inhibitors in Ewing sarcoma. As a single agent, there is some activity in Ewing sarcoma cell lines and a highly statistically significant relationship between olaparib sensitivity and EWS–FLI1 expression. Howev
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bazedoxifene While previously reported optimizations on comp
2021-04-17
While previously reported optimizations on bazedoxifene focused on the phenyl ring A () and substituents on isoxazole ring, other alternatives to replace isoxazole ring were never explored. Herein, we propose to replace the isoxazole with its bioisosteric substituted phenyl ring B () to explore ne
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br Introduction Epithelial mesenchymal transition EMT
2021-04-17
Introduction Epithelial-mesenchymal transition (EMT) is a biological process by which epithelial 15 lose cell polarity and cell-cell adhesion, and gain mesenchymal features with an increase of migratory and invasive properties [1]. EMT is essential for mesoderm formation during embryo developmen
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The yeast Rad p radiation sensitive also called
2021-04-17
The yeast Rad6p (radiation sensitive 6, also called Ubc2) E2 ubiquitin-conjugating enzyme is a member of the highly conserved UBC proteins in eukaryotes (Xu et al., 2009). Rad6p is involved in several cellular processes, including DNA repair, transcriptional activation and silencing, histone ubiquit
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A spectrum of therapies came in order
2021-04-17
A spectrum of therapies came in order to counter this misfortune, some of them are discussed below. However, the common problem faced by most of these drugs is their emerging resistance after a span of time. Some of the important drugs reported so far are as: Quinine-based antimalarial drugs (Fig. 1
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br Inhibition of DHODH The final products a n were
2021-04-17
Inhibition of DHODH The final products 7a–n were assessed for their DHODH inhibitory activity on rat liver mitochondrial/microsomal membranes. A procedure adapted from the literature was employed (see Experimental), in which oxidation of DHO to ORO is monitored by following the concomitant reduct
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