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br Oxidoreductase like MEM for prodrug activation br
2021-05-10
Oxidoreductase-like MEM for prodrug activation Future outlook Although MEM-mediated prodrug activation has been performed by different MEMs and prodrugs, and their effectiveness have been proved in vivo, only a few types of MEMs or prodrugs have been explored in prodrug activation until now [2
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In contrast a single instillation of
2021-05-10
In contrast, a single instillation of BLM results in a progression of inflammatory events that culminates in marked remodeling of the lung interstitium. This process takes 2–3 weeks, with the fibrotic lesions becoming most pronounced within the first month [9]. Consequently, the BLM model offers the
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At present there have been
2021-05-10
At present, there have been relatively few studies that evaluated potential correlations between pulmonary and pleura metastases, hilar and mediastinal benzydamine nodes, and organs associated with distant metastasis and EGFR mutations [33,34,37]. Further research on these relationships is needed,
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In the case of the reaction of a with
2021-05-10
In the case of the reaction of 1a with Py2SMeCu(II), compound 4a was observed as the major oxidation product suggesting that further oxidation or hydrolysis of 4a was prevented under our conditions. The precise factors that govern the reactivity and stability of nitrosoamidines remain poorly known.
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Herein the interactions of etamicastat
2021-05-10
Herein, the interactions of etamicastat, nepicastat and zamicastat with P-gp and BCRP were evaluated. Although recent investigations have been performed to assess the involvement of P-gp in the Alogliptin synthesis exposure of nepicastat and etamicastat (Loureiro et al., 2015), the contribution of B
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Except for S adenosylmethionine SAM Fig sources
2021-05-10
Except for S-adenosylmethionine (SAM, Fig. 1), sources of endogenous DNA alkylation are not well defined. Other possible sources include nitroso compounds related to the well known mutagen methylnitrosourea which are generated in vitro by nitrosation of cellular amines including amino acids, protein
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br Introduction In mammals there are ten known isoforms
2021-05-10
Introduction In mammals there are ten known isoforms of the enzyme diacylglycerol kinase (DGK), as well as gene splice variants. Enzymes of this family all have a homologous active site but differ widely in their molecular mass, mechanisms of activation and biological function (Shulga et al., 201
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The combination of brequinar and fluorouracil FU has been ev
2021-05-10
The combination of brequinar and 5-fluorouracil (5-FU) has been evaluated to assess whether brequinar-induced uridine depletion would improve 5-FU activity. In cells, 5-FU is metabolized into FdUMP and inhibits thymidylate synthetase, which catalyzes the formation of thymidine monophosphate from deo
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A range of therapies exists
2021-05-10
A range of therapies exists for the treatment of inflammation-driven diseases, which can be summarized as non-steroidal anti-inflammatory drugs (NSAIDs), corticoids and steroidal-related drugs (Ward et al., 2008). Despite of these notable successes, there are still major unmet medical needs in the t
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Since free testosterone diffuses into a target organ a remar
2021-05-10
Since free testosterone diffuses into a target organ [1], a remarkable increase in free testosterone in plasma is expected to enhance androgen response in target organs including the prostate. In fact, the results of the present study showed testosterone and DHT levels, and mRNA expression levels of
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Common to all models for nuclear transport is the
2021-05-10
Common to all models for nuclear transport is the binding of importins/exportins to FG repeats found in about a third of the ∼30 nucleoporins, the so-called FG-Nups (Iovine et al., 1995, Rexach and Blobel, 1995); for review, see Grossman et al. (2012), Stewart (2007), and Terry and Wente (2009). FG-
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Dopamine activity in the PFC and striatum
2021-05-08
Dopamine activity in the PFC and striatum may be antagonistic, meaning that lower levels of dopamine in the striatum tend to correspond to higher levels of dopamine in the PFC and vice versa (Cools and D'Esposito, 2011; Tunbridge et al., 2006). Human PET studies have reported that dopaminergic PFC f
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Synthetic peptides have proven highly valuable
2021-05-08
Synthetic peptides have proven highly valuable in replicating the characteristics of collagen and in defining the sites on collagen essential for binding and studying protein–collagen interactions. There are, however, disadvantages to synthetic collagen-like peptides. First, the thermal stability of
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Our observation that nuclear but not cytoplasmic EP
2021-05-08
Our observation that nuclear, but not cytoplasmic EP4 expression is associated with different outcomes is interesting. In breast cancer, using the same methods, we did not detect EP4 in the nucleus of malignant herpes simplex virus 1 whereas cytoplasmic EP4 was commonly observed [13]. While G prote
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We had earlier reported that collagen fibers with
2021-05-08
We had earlier reported that collagen fibers with intact native banded structure were occasionally observed in the kinase-deficient, membrane-anchored DDR2 ECD (DDR2/-KD) samples; however, in our DDR1/ECD and DDR2/ECD samples, observation of native banded structure of collagen was far more infrequen
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