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Introduction Prolyl hydroxylation is a widely observed
2020-12-24
Introduction Prolyl hydroxylation is a widely observed post translational modification in collagen, an abundant animal protein. The high content (~13% per chain of the triple helical structure) of 4-hydroxyproline (Hyp,O) in collagen, togather with the natural abundance of collagen has led to the e
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To simulate the inhibition of the
2020-12-24
To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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As mentioned above disruption of Tgif
2020-12-24
As mentioned above, disruption of Tgif1 in mice is associated with dyslipidemia, and here we investigate the effects of overexpression of TGIF1 on expression of the Npc1l1 gene and markers of intestinal cholesterol absorption. Materials and methods Results Discussion In this study, we soug
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We observed the IVM potentiation of currents induced
2020-12-24
We observed the IVM potentiation of currents induced by the EC5 of Glu or GABA and the IVM inhibition of currents induced by the EC90 of Glu or GABA in wild-type GluCls and GABACls. The EC50 of IVM for the potentiation in GluCls was 3.5-fold smaller than that in GABACls (Fig. 4, Fig. 8B, Table 2), a
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ET expression occurs in many carcinomas
2020-12-24
ET-1 expression occurs in many carcinomas, including those arising in the kidney [38], prostate [7], ovary [5] endometrium [39], melanocyte [40], and central nervous system [41], [42], among others [43]. The endothelin axis expression in RCC appears to be dependent upon the tumor subtype [38]. In se
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br Most reported binding data are
2020-12-24
Most reported binding data are obtained by performing heterologous competition binding experiments and expressing the results as relative binding affinity (RBA). The constructed binding curves should theoretically be sigmoidal in shape with a Hill slope value of one, for a single ligand binding to
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Tibolone is also efficacious on
2020-12-24
Tibolone is also efficacious on bone in elderly women and induces a clear reduction in bone turnover markers [50], [51]. Rymer et al. showed that, after 10 years of treatment with tibolone, the difference in bone mineral density compared with a placebo group was more than 12% for both lumbar spine a
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In countries such as China
2020-12-24
In countries such as China where there is a high commercial production of rice, the use of rice husk ash (RHA) as an alternative cementing material can become a great asset for environmental rehabilitation and address the difficult disposal issues associated with this agricultural waste [23]. RHA po
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ERR is expressed in several adult and embryonic tissues but
2020-12-24
ERRγ is expressed in several adult and embryonic tissues but its biological role is still largely unknown [21]. Overexpression of ERRγ in breast cancer correlates with a favorable outcome [22]. In addition, ERRγ has been reported to inhibit the growth of prostate tumor p2y receptor [23]. In this st
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Key molecules in the EP
2020-12-24
Key molecules in the EP1 second messenger signaling cascade that are necessary for potentiation of GluK2/GluK5 were identified. We also identified three GluK5 serines located in a membrane-proximal C-terminal domain that, when mutated to the phosphomimetic aspartate and expressed with GluK2, rendere
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Covalent inhibitors are well suited for targeting
2020-12-24
Covalent inhibitors are well suited for targeting the E1 lp-pla2 of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in circula
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Potential break through technology poised to overcome these
2020-12-24
Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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Introduction Glucose is the major carbon source in
2020-12-24
Introduction Glucose is the major carbon source in most organisms. Cancer IMD 0354 in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammals is mainly media
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br Introduction Cerebral stroke causes an efflux
2020-12-24
Introduction Cerebral stroke causes an efflux of various groups of progenitor and stem cells from bone marrow to bloodstream and the levels of these cells correlate with neurological status of stroke patients (Gójska-Grymajło et al., 2012, 2018). It is thought that paracrine factors produced by t
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In the phase I AURA trial patients with EGFR activating
2020-12-24
In the phase I AURA trial, patients with EGFR activating mutations and centrally confirmed tumor and/or plasma genotyping (BEAMing) T790M result were enrolled. Among 216 patients with both plasma and tissue genotyping results, the concordance rate was 82% for fty720 19 deletions, 86% for L858R and
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