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hiv integrase inhibitor As part of a program to explore the
2020-03-24
As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substitu
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k145 br Discussion The present results
2020-03-24
Discussion The present results demonstrate that high dose estrogen–progestogen OC treatment produced impaired glucose tolerance and glucose tolerance was preserved during low dose estrogen–progestogen, high or low dose progestogen-only OC use. The study also shows that impaired glucose tolerance
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Interestingly anti inflammatory actions for
2020-03-24
Interestingly, anti-inflammatory actions for sPLA2-V were also described in mice a few years ago in a model of autoimmune complex mediated arthritis [148]. A novel mechanism was delineated, whereby sPLA2-V promotes phagocytosis of immune complexes by macrophages to ameliorate inflammation in autoimm
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br Materials and methods br
2020-03-24
Materials and methods Results Discussion Ubiquitination is an important eukaryotic process that defines the fate of proteins and their functionality. It has multiple roles in cell survival, differentiation and development (Glickman and Ciechanover, 2002). Ubiquitination is usually known as
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Abdominal aortic aneurysm AAA is considered a major health c
2020-03-24
Abdominal aortic aneurysm (AAA) is considered a major health concern and is associated with extremely high rates of mortality in case of aortic rupture. The main pathophysiologic mechanisms leading to aortic dilation include the degradation of the extracellular matrix (ECM) components, such as colla
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The aberrant methylation of genes
2020-03-24
The aberrant methylation of genes that suppress tumorigenesis appears to occur early in tumor development and increase progressively, eventually leading to the malignant phenotype [35]. Genes involved in every step of tumorigenesis can be silenced by this epigenetic mechanism. Hypermethylation of pr
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br Funding sources br Introduction Psychiatric comorbidities
2020-03-24
Funding sources Introduction Psychiatric comorbidities affect up to 70% of people with pharmacoresistant epilepsy and significantly impact quality of life [1]. Psychiatric comorbidities in epilepsy have been thought to be due to psychosocial stress. However, recent evidence suggests a more com
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MKT 077 The immune control of CMV replication in vivo
2020-03-24
The immune control of CMV replication in vivo is primarily driven by the T-cell-mediated response, a characteristic that has been proposed as a tool to individualize and therefore to optimize antiviral treatment [6], [7], and it has been associated with spontaneous clearance of CMV viraemia in patie
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Antioxidants such as SFN have been proposed to be
2020-03-24
Antioxidants such as SFN have been proposed to be chemopreventive agents to inhibit, delay or reverse the development of cancer (Bayat Mokhtari et al., 2018). SFN was shown in breast epithelial cell culture to suppress oxidative metabolism of E2/E1 and thus protect against estrogen-mediated DNA dama
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In S cerevisiae Mek a paralog of the checkpoint
2020-03-24
In S. cerevisiae, Mek1, a paralog of the checkpoint kinase Chk2, mediates cell-cycle arrest in response to meiotic defects (Bailis and Roeder, 2000, Xu et al., 1997). Mek1 is associated with meiotic chromosome axes, where its activation requires interactions with two other axis proteins, Hop1 and Re
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br Materials and methods br
2020-03-23
Materials and methods Results We examined the effects of curcumin in Fluo-4 loaded SH-EP1 Neurotensin receptor stably transfected with human α7-nACh receptor. Application of curcumin alone in the concentrations up to 100 μM for 30 sec. did not induce any detectable change in intracellular Ca2
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From the general synthetic route we first synthesized a dire
2020-03-23
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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Carbazole could be recrystallised from
2020-03-21
Carbazole could be recrystallised from ethyl acetate to provide bright red crystals suitable for single crystal X-ray diffraction (see ). The first crop showed had crystallised preferentially as the ()-isomer (A). Examining the single crystal X-ray data of it was interesting to find that the N2C15 b
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Thus the understanding of the various mechanisms of
2020-03-21
Thus, the understanding of the various mechanisms of action of estrogen and SERMs is an important medical challenge and could help to develop an “ideal” SERM, preserving the beneficial effects of estrogen in the bone and urogenital system, and reducing the unwanted side effects, mainly increased ris
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br Effects of estrogen on
2020-03-21
Effects of estrogen on vascular function Atherosclerosis is a chronic inflammatory condition of the vascular wall (Figure 1) that can be converted to an acute clinical event by the induction of plaque rupture or erosion, leading to thrombosis [58]. This perpetuating process is characterized by ph
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