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Several main strategies for targeting E s described in
2021-04-21
Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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The first hint that GLP might
2021-04-21
The first hint that GLP-1 might not be completely stable came from a meeting abstract in 1992, reporting that GLP-1 could be degraded in plasma incubations [16], although the enzyme(s) involved was not identified. A year later, Mentlein and colleagues [17], in a search for peptide substrates of the
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jnk pathway br Introduction Pattern separation is the
2021-04-21
Introduction Pattern separation is the ability to make distinct representations from highly overlapping information, a process which is important for memory encoding (Clelland et al., 2009). For correct pattern separation, old information needs to be retrieved and compared to new information. If
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Since the initial identification of DNA
2021-04-21
Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the
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We therefore propose a scenario based on our experimental
2021-04-21
We therefore propose a scenario based on our experimental models and depicted schematically in Figure 7. In fully respiring cells, CI, CII, and DHODH transfer electrons to CoQ, which are then forwarded to CIII. This latter complex transfers electrons to CIV, which then produces water at the expense
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br Application of the screening system for ITP binding prote
2021-04-21
Application of the screening system for ITP-binding proteins Inosine is a nucleoside with hypoxanthine as a base. Inosine nucleotides are relatively abundant in human SR3335 because inosine monophosphate (IMP) is a general precursor molecule for the de novo synthesis of AMP and GMP or a product o
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The IP R is a ubiquitously expressed
2021-04-21
The IP3R is a ubiquitously expressed Ca2+-release channel from the ER, activated by IP3, produced upon cellular stimulation by hormones, growth factors or neurotransmitters. Three genes are coding for the IP3R and their gene products (IP3R1, IP3R2, IP3R3) assemble in functional homo- or heterotetram
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Here we found that these leukotriene
2021-04-21
Here we found that these leukotriene antagonists also inhibit the effects of nucleotides acting at P2Y receptors in dU937 cells, which are known to express a number of nucleotide receptors, such as P2Y2 or P2Y4[30]. In an effort to characterize the P2 receptor subtypes subject to negative modulation
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During DNA replication p protein
2021-04-21
During DNA replication p21 protein binds PCNA, in its role as processivity factor, to stop replication when there is DNA damage, and apparently p21 also binds PCNA when this is in complex with Cyc/CDKs [11]. In plants, KRPs (functional analogs of p21), inhibit kinase activity in CycD/CDKs complexes
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Many authors have described the existence of correlation bet
2021-04-21
Many authors have described the existence of correlation between viability and moisture content and therefore, water availability. Sabuquillo et al. (2010) demonstrated that only Penicillium oxalicum conidial formulations whose initial moisture contents ranged between 5 and 14% retained their viabil
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Our results for imidacloprid were unexpected
2021-04-21
Our results for imidacloprid were unexpected: considering that imidacloprid (Im) is a neonicotinoid insecticide with a different mode of action (agonist of the nicotinic ak7 receptor) than OPs, we expected Es-ChE and T-ChE activity to be largely insensitive to changes in Im concentrations. However,
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In contrast to drospirenone dydrogestrone acts rather neutra
2021-04-21
In DASA-58 to drospirenone dydrogestrone acts rather neutral at the aldosterone-, glucocorticoid- and androgen-receptor [12]. This indicates that the assessment of a ‘net-overall effect’ on the vascular system is very difficult based on the often discussed ‘partial effects’ of the progestogens. Thu
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Thus the understanding of the various mechanisms of
2021-04-21
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 The estrogen receptors History and
2021-04-21
The estrogen receptors: History and discovery In 1958, Elwood Jensen discovered the estrogen receptor, the first receptor ever encountered for any hormone, by showing that reproductive female tissues were able to uptake estrogen from the circulation by binding to proteins. He later demonstrated t
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Fisetin tetrahydroxyflavone is a flavonol present in several
2021-04-20
Fisetin (3,3′,4′,7-tetrahydroxyflavone) is a flavonol present in several fruits and vegetables such as grape, persimmon, strawberry, apple, and onion at concentrations rangeing from 2 to 160 μg/g. Fisetin is a well–known bioflavonoid with remarkable biological effects including chemopreventive/chemo
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