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A summary of the drug CDK hydrophobic hydrogen bonding H
2021-06-17
A summary of the drug-CDK2/6/9 hydrophobic (Φ), hydrogen-bonding (H), and polar-bonding (P) interactions based upon the KLIFS residue numbers is provided in Table 5. The KLIFS system gives comparable residues from different azacytidine the same value [77], which facilitates comparisons among differe
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Acidic substituents showed moderate biochemical activity but
2021-06-17
Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic how to calculate mmol were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their b
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This study evaluated the role of SERT
2021-06-17
This study evaluated the role of SERT in classical fear conditioning using a SERT knockout rat model. We found a clear disruption of cue-conditioned fear in SERT−/− rats, as measured with the fear-potentiated startle. This disruption was due to a deficit in fear acquisition and was accompanied by de
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Neuroinflammation is the one of
2021-06-17
Neuroinflammation is the one of the emerging causal factors contributing to these cognitive deficits. Therefore, we further tested the hypothesis that neuroinflammation is a key component contributing to the progression of spatial memory deficits during HH. Spatial memory deficits were observed afte
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br Introduction The endeavor to achieve a
2021-06-17
Introduction The endeavor to achieve a successful use of commercial-off-the-shelf (COTS) electronic devices in space is not new and the reasons are well known [1], [2], [3]. More recently, COTS have been widely employed in the manufacturing of low-cost, small satellites, for scientific and even c
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Introduction Safety critical systems are defined
2021-06-17
Introduction Safety-critical systems are defined as those systems where failure could result in the loss of life or injury to people, damage to equipment or to the environment [9]. Safety standards, e.g., [41], [17], [18], [6], [38], expect appropriate safety analysis tasks to be integrated within
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Collectively these data suggest the potential clinical
2021-06-17
Collectively, these data suggest the potential clinical utility of COMT inhibitors for the treatment of addiction disorders. Similar to current pharmacotherapies such as naltrexone, tolcapone's effects were not ethanol specific, therefore tolcapone may be effective in reducing other drug reinforced
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Bearing in mind that temperamental traits are
2021-06-17
Bearing in mind that temperamental traits are genetically determined, in the present study we have chosen to investigate COMT and OPRM1 gene polymorphisms related to stimulation of the nervous system, which is extremely important in combat sports. The μ-opioid receptor gene OPRM1 is located on the
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In rodent models the loss of estrogens
2021-06-17
In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an T-5224 receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitric oxide synthase inhibi
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Although it is well established that
2021-06-17
Although it is well established that estrogen and ESR1 mediate numerous reproductive processes, increasing evidence suggests that ESR2 also lays an integral role in reproduction. ESR2 is a mediator in folliculogenesis and may also act by stimulating ovulation and regulating luteinization (Su et al.,
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Oleandrin br Inhibiting APC C during Interphase and
2021-06-16
Inhibiting APC/C during Interphase and prior to Anaphase Because ubiquitylation by APC/C triggers cell division, it is essential that APC/C is restrained until cells are prepared for its substrates to be degraded. In addition to regulation by phosphorylation, an additional layer of control comes
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The synthesis of compounds a
2021-06-16
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of U0126 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b were obtai
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A spectrum of therapies came in order to counter
2021-06-16
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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Funding sources This study was funded
2021-06-16
Funding sources This study was funded by European Community’s Seventh Framework Programme under grant agreement No. 305662 (Project: Community-based scheduled screening and treatment of malaria in pregnancy for improved maternal and infant health: a cluster-randomized trial ‘COSMIC’). Acknowledg
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br Contributors br Acknowledgements br
2021-06-16
Contributors Acknowledgements Introduction Pemphigus disorders are characterized by autoantibodies binding to desmosomes between epidermal cells, resulting in the loss of cell to cell adhesion and blister formation. In pemphigus foliaceus, autoantibodies predominantly bind to desmoglein 1,
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