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br Early developments Historically the advent of SMEPT
2019-08-26

Early developments Historically, the advent of SMEPT can be traced to the 1980′s, where the first example of localized prodrug conversion was achieved using a judiciously placed enzyme – in order to achieve a localized feed of 5-fluorouracil (5-FU). Immobilization of E. coli-derived cytosine deam
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br Acknowledgments br Introduction Ubiquitin ligases limit
2019-08-26

Acknowledgments Introduction Ubiquitin ligases limit the stability and activity of substrates by targeting them for proteasomal-dependent degradation. Siah is a two-member family of ubiquitin ligases implicated in control of key cellular processes. Among those, Siah ligases control prolyl hydr
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UBA belongs to the non canonical E enzymes that lack
2019-08-26

UBA5 belongs to the non-canonical E1 enzymes that lack a defined Cys domain but have the active-site Cys within the adenylation domain [24]. Similar to other E1 enzymes, UBA5\'s adenylation domain comprises an eight-stranded beta sheet that is surrounded by helices [21]. Moreover, like the ancestral
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Eleutherococcus senticosus Rupt Maxim Maxim is a shrub belon
2019-08-26

Eleutherococcus senticosus (Rupt. & Maxim.) Maxim is a shrub belonging to the Araliaceae, which is commonly distributed in China, Korea, Japan and Russia. It has been traditionally used as folk medicine for the treatment of rheumatism, diabetes, and hepatitis (Nan et al., 2004). Recent phytochemical
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br Conclusion The results of the present study demonstrate t
2019-08-26

Conclusion The results of the present study demonstrate that cysteinyl leukotrienes LTC4, LTD4 and LTE4 cause moderate to marked whereas the dihydroxy leukotriene LTB4 causes small muscle contraction in the stomach in vitro. The LTD4-induced contraction is mediated by CysLT1 in fundus but by CysL
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In rats exposed to day of nicotine withdrawal h
2019-08-26

In rats exposed to 1 day of nicotine withdrawal (24 h after the last nicotine administration) we expected a decrease of general locomotor activity and a decrease of global striatal dopamine release, which were assessed in a previous study following 14 days of nicotine exposure and 24 h of nicotine w
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Taking into account that Gr dysfunction is involved in
2019-08-26

Taking into account that Gr dysfunction is involved in the molecular mechanisms underlying HPA axis disorder (Li et al., 2017b) and Gr activity has been reported to be lowered in patients with severe mood disorders (Rush et al. 1996) and in adult rats (Green et al. 2016), PFOS could alter HPA axis a
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Beside the previously reported Topo I inhibition
2019-08-24

Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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During the Lapita period in Tonga
2019-08-24

During the Lapita period in Tonga, the Talasiu site would have been an attractive location for human settlement as it overlooked an embayment holding large numbers of sessile and gregarious shellfish close to a fresh water solution channel, with gardening soils immediately inland. However, sea level
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Interestingly selective ETA blockade increased cutaneous blo
2019-08-24

Interestingly, selective ETA blockade increased cutaneous blood flow as measured by laser Doppler fluxmetry. This is a measure of total blood flow in the different vessels in the skin including venules, lipid metabolism pathway as well as arterioles. This finding is in accordance with the previous
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One possibility to differentiate between the two failure
2019-08-24

One possibility to differentiate between the two failure modes, and also to identify the corresponding characteristics of the resulting fracture surface, is a series of FNCT measurements with varying nominal (initial) stress. The dependence of the observed time to failure tf on the actual stress cha
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br Introduction Our understanding of how
2019-08-24

Introduction Our understanding of how ligands interact with G protein coupled receptors is evolving, particularly the recognition that some have the ability to preferentially activate a subset of intracellular signalling cascades – so called pathway biased ligands [1]. Additionally, it is now acc
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It is believed that emphysema in smokers
2019-08-24

It is believed that emphysema in smokers is mediated by proteases released from inflammatory LB42708 that cause destruction of the extracellular matrix in alveolar septa [1]. Metalloprotease-12 is mainly released by macrophages and is considered the enzyme responsible for emphysematous lesions in e
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All DGKs have at least
2019-08-24

All DGKs have at least two cysteine-rich regions homologous to the C1A and C1B motifs of PKCs [26]. In theory, these domains may bind DAG, perhaps localizing DGKs to where DAG accumulates. However, no DGK C1 domain has so far been conclusively shown to bind DAG. In fact, structural predictions sugge
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CGP 54626 hydrochloride In vasculature NADPH oxidases NOXs a
2019-08-23

In vasculature, NADPH oxidases (NOXs) are the main sources of O2− generation that involve in the transfer of electrons to molecular oxygen. Endothelin-1 [25] and thromboxane A2 [26] were reported to induce eNOS uncoupling via upregulation of NOXs. Additionally, inhibition of p47 phox, a subunit of N
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