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p Kip is a critical component of the cell cycle
2021-06-15
p27Kip1 is a critical component of the cell cycle machinery [15]. As an inhibitor of cyclin E-Cdk2, p27Kip1 plays a pivotal role in controlling cell proliferation, S-phase entry, and G1-phase exit during development and tumorigenesis [16]. p27Kip1 is predominantly regulated via posttranslational mod
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br Materials and methods br Results br Discussion In this
2021-06-15
Materials and methods Results Discussion In this study, we investigated two novel candidate therapeutics, the related CRM1-inhibiting SINEs KPT-185 and KPT-276, in treatment of NHL. The results showed that KPT-185 induced growth inhibition, cell-cycle arrest, and apoptosis in tumor Labetalo
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In recent years neuroimaging studies have increasingly demon
2021-06-11
In recent years, neuroimaging studies have increasingly demonstrated acute effects of THC on Azithromycin function, the vast majority of them involving a cognitive challenge (Bossong et al., 2014b). For example, without affecting performance accuracy, THC caused reductions in activity during encodin
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The second part of this study evaluated
2021-06-11
The second part of this study evaluated the role of CK1 in the eFABP4 cellular uptake in endothelial cells. By blocking CK1 expression using a specific siRNA, we corroborated that the presence of CK1 was fundamental for FABP4 cellular uptake and internalization in endothelial cells, thus decreased m
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For membrane protected SPE the
2021-06-11
For membrane protected μ-SPE, the choice of sorbent is crucial because it determines the extraction efficiency. Up to now, many porous materials, such as carbon based sorbents [1,[3], [4], [5], [6]], ethylsilane or octadecylsilane modified silica (C2 or C18) [7,8], polymeric materials [[9], [10], [1
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Research done thus far supports the hypothesis that MPA
2021-06-11
Research done thus far supports the hypothesis that MPA has detrimental effects on cognition, alone and in combination with estrogen; there are other FDA-approved progestogens that satisfy the uterus opposing effects that have not been cognitively profiled. An important goal to aid women's health is
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In our former work our
2021-06-11
In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b
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As illustrated in Table monocyclic acid analogs were synthes
2021-06-11
As illustrated in Table 3, monocyclic corticotropin releasing factor analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one analog 9
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Initially we ascertained that if the dose
2021-06-11
Initially, we ascertained that if the dose of elastase was sufficient to cause pulmonary emphysema, then pulmonary emphysema could be maintained throughout the study. We found that elastase at 3U was sufficient to cause emphysema that remained over 35 days. In this experimental design of lung diseas
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NT157 Both the kK and kK mediated ubiquitination leads to ra
2021-06-11
Both, the kK3 and kK5-mediated ubiquitination leads to rapid internalisation of target proteins followed by lysosomal degradation, similar to that seen for MARCH-1/8 [77]. Ubiquitination activity of kK3 and kK5 depends on the positioning of the targeted lysine (or cysteine) residues [22]. The positi
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A prominent example of such
2021-06-11
A prominent example of such enzyme is the proteasome, a highly promising target not only in cancer, but also in inflammatory and autoimmune diseases. Circulating proteasomes and respective anti-proteasome autoantibodies were detected in serum samples from patients with autoimmune diseases such as mu
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Protein degradation via UPP involves two steps One step
2021-06-11
Protein degradation via UPP involves two steps. One step is the conjugation of multiple ubiquitin to a substrate. The other step is the degradation of tagged protein by the downstream 26S proteasome complex. Protein ubiquitination is the E1–E2–E3 enzymatic cascade (Hershko & Ciechanover, 1998). E1-a
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br Conclusions and future directions In
2021-06-11
Conclusions and future directions In recent years we saw major advances in our knowledge of H2A-DUB biology, with discovery of novel mammalian H2A-DUBs, better understanding of their biochemical properties, and development of several animal models to address their in vivo functions. However at pr
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The folate pathway plays an essential role in cell survival
2021-06-10
The folate pathway plays an essential role in cell survival by generating 5, 10-methylene tetrahydrofolate as a one-carbon donor for the synthesis of deoxythymidine monophosphate (dTMP), purines, methionine and histidine. Disruption of this pathway leads to the critical deficiency of these key molec
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The aniline R group was extensively explored and
2021-06-10
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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