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The compounds were ranked based on the Glide
2020-11-25

The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR a
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Tenovin-1 br Conflicts of interest br Introduction Diacylgly
2020-11-25

Conflicts of interest Introduction Diacylglycerols (DAGs) and phosphatidic Tenovin-1 (PA) play fundamental roles in biology as basic components of membranes, intermediates in lipid metabolism, and secondary messengers in cellular signaling (Carrasco and Merida, 2007, Fang et al., 2001). Cells
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Multiple sequence alignment of the proteins
2020-11-25

Multiple sequence alignment of the proteins in the DGAT1 sub-family shows that there are about 41 conserved amino LY2584702 residues distributed over seven sequence motifs [74]. Unlike DGAT2, a large number of DGAT1 residues, including a majority of the conserved residues, are found in a loop on th
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The authors gratefully acknowledge financial
2020-11-25

The authors gratefully acknowledge financial support from the State of São Paulo Research Foundation (FAPESP, Fundação de Amparo à Pesquisa do Estado de São Paulo), grants 2013/07600-3 and 2013/25658-9, and the National Council for Scientific and Technological Development (CNPq, Conselho Nacional de
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br Material and methods br
2020-11-25

Material and methods Results Discussion Monomeric CDK5 shows no enzymatic activity and requires the association with a regulatory partner for activation (Dhavan and Tsai, 2001). Here, we found that CDK7 might be one of the partners required for activation of CDK5 in the skin tissue, based o
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One strategy which is different from
2020-11-24

One strategy which is different from the above is to isolate a similar enzyme to the one under study which will not be recognized by the antibody of the original protein. This approach will lead to prolonging an enzyme’s activity. For example, a novel variant of Carboxypeptidase G2 (CPG2), which has
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Cancer has been linked to
2020-11-24

Cancer has been linked to both genetic and epigenetic changes. Epigenetic modifications, mainly DNA methylation at CpG dinucleotides, affect the regulation of gene transcription without altering the gene's sequence. Short sequences rich in CpG dinucleotides (i.e., CpG islands) are often found in the
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Our study has several limitations As this study was
2020-11-24

Our study has several limitations. As this study was performed at a single institution, it had a limited sample size and was not powered to detect specific differences in assay performance by organ group or waitlist status. In the two CMV seropositive subjects with potential passive antibodies, the
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br Discussion Immune response to CMV is
2020-11-24

Discussion Immune response to CMV is a series cell-mediated immune response initiated by innate innate NK cells, followed by adaptive CD8+ and CD4+ T cells and humoral immunity by B cell [3]. Prior to transplant, measurement of humoral immune responses (CMV serology) of donor and recipient is com
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Another layer of CK regulation
2020-11-24

Another layer of CK1 regulation in the Hh and Wnt pathways is to employ different CK1 isoforms to phosphorylate distinct pathway components or even distinct sites on the same substrates. In this regard, it has been shown recently that the membrane-associated CK1 isoform CK1γ, but not the cytosolic i
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In summary A is a potent orally
2020-11-24

In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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beta amyloid cAMP mediated signaling pathways are important
2020-11-24

cAMP-mediated signaling pathways are important for maintaining metabolic homeostasis, and the effects of the glucagon/catecholamine–cAMP–PKA axis on energy balance have been well documented [20]. For example, beta amyloid of the PKA 2β regulatory subunit (RIIβ) in mice leads to increased expression
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Anaesthetized mice of one eNOS KO strain showed a paradoxica
2020-11-24

Anaesthetized mice of one eNOS-KO strain showed a paradoxical decrease in blood pressure (BP) in response to i.p. administration of the NOS-inhibitor L-NA suggesting a role for non-endothelial isoforms of NOS in maintaining BP [1]. Alternatively, diminution in the activity of the renin-angiotensin s
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It is known that cigarette
2020-11-24

It is known that cigarette smoke increases the oxidative burden in the lungs of mice with emphysema, which leads to oxidative stress [[34], [35], [36]]. However, in addition to cigarette smoke, studies have shown that endogenous oxidative stress is associated with proteolytic Methotrexate in severa
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Because sex steroids and growth hormone play an
2020-11-24

Because sex steroids and growth hormone play an important role in the development and maintenance of hepatic CYP450 enzyme expression and ER expression, it is possible that exposure to endocrine active agents during gestation and perinatally could alter expression of these proteins. Therefore, these
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