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Three dimensional conformational changes in the
2020-10-13
Three-dimensional conformational changes in the cargo protein’s NES, caused by protein phosphorylation, dephosphorylation, or mutation, can regulate CRM1 binding (Craig et al., 2002, Vogt et al., 2005). Additional protein modifications such as sumoylation, ubiquitination, acetylation, and/or the bin
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Within the Class II receptors
2020-10-13
Within the Class II receptors, the Type I IFN receptor subunit, IFNAR-1, is exceptional in having four tandem FNIII domains, denoted here D1–D4. This structure appears to have arisen as a tandem glucose transporter of the basic D1/D2 structure; thus, D1 and D3 of IFNAR-1 are more closely related, a
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Various domains of the HSA
2020-10-12
Various domains of the HSA molecule have also been used to make bioconjugates with increased stability, better targeting properties, and/or extended half-lives in blood. For example, domain I of HSA has been used in the preparation of antibody conjugates. This was achieved through the use of a cyclo
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Hexamethonium Bromide Introduction We have recently identifi
2020-10-12
Introduction We have recently identified that caseinkinase 2 (CK2) inhibition protects white matter (WM) from ischemic injury. We focused our research on CK2 because upregulation of CK2 activity is associated with many diseases, including ischemic injury [1,[6], [7], [8]]. This review highlights an
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A possible explanation for these observations has been provi
2020-10-12
A possible explanation for these observations has been provided by a recent study showing that EWS-FLI-1 increases the Skp2-mediated 26S proteasome degradation, decreasing p27 protein stability and preventing cell senescence [42]. Mechanism of action of EWS-FLI-1 Molecular analysis has revealed
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The Acat gene was identified by
2020-10-12
The Acat1 gene was identified by functional complementation of a Chinese hamster ovary cell mutant lacking ACAT activity [12]. Unlike most other genes, human Acat1 is located in two different chromosomes, HU 308 1 and 7, with each site containing a distinct promoter: chromosome 1 contains exons 1–1
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Judging from the densitometric analysis
2020-10-12
Judging from the densitometric analysis of the Western blots, CYP2E1 protein was expressed, although at very low levels, by PT cells. This corresponds to previous observations [10], showing that CYP2E1 was expressed in the PT, although expression was higher in the distal tubule. Testosterone 6β-hyd
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In the current study cocaine
2020-10-10
In the current study, cocaine did not significantly increase negative subjective effects and nepicastat did not increase these responses. This outcome is somewhat surprising given that the most commonly reported effect to date has been to increase the aversive properties of cocaine such as anxiety,
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Our study showed that parental morphine exposure in the
2020-10-10
Our study showed that parental morphine exposure in the adulthood is associated with an increased tendency toward morphine consumption in F1 but not F2 male offspring. Thus, it seems that trans-generational effects of parental morphine consumption disappear in the second generation. In support of ou
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Recent studies from the literature have identified new
2020-10-10
Recent studies from the literature have identified new calcium ionophore of antiviral agents able to target diverse host factors indispensable for efficient virus replication: as an example, the human DEAD-box polypeptide 3 (DDX3) inhibitor, 1-[4-(4-methyl-1H-1,2,3-triazol-1-yl)phenyl]-3-o-tolylurea
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Classical DHFR inhibitors such as methotrexate
2020-10-10
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Z-IETD-FMK residues as well as hydrophobic
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Xifaxan Such concerns do not apply to the
2020-10-10
Such concerns do not apply to the anti-inflammatory actions shown by the agent, given that CR3465 proved effective in various models of inflammation including guinea pig, rat, and human. Airway inflammation, involving a complex network of local mediators, cytokines, and effector Xifaxan (Bradley et
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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2020-10-10
Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase Pyrene azide 3 [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour and
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The present review also summarizes the efforts that have bee
2020-10-10
The present review also summarizes the efforts that have been made to find new c-FMS inhibitors under clinical trial as given in the Table 1. These inhibitors may reduce the burdens of potency and side effects that have faced the scientists globally. ABT-869 41 was manufactured in Abbott laboratorie
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As previously stated the most unexpected finding
2020-10-10
As previously stated, the most unexpected finding from this series of compounds was the identification of a dimethyl isoxazole side chain that gave dramatically improved binding over the parent compounds. Holding this piece of the molecule constant, a series of analogs were made to further understan
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