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The exact mechanism by which
2022-04-15
The exact mechanism by which mitochondrial hexokinases such as HK1 and HK2 prevent apoptosis is unclear. Mitochondrial hexokinases have been shown to bind with the voltage-dependent anion channel 1 (VDAC1), giving them direct access to ATP for use as an energy source [36]. Akt has been shown to prom
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Several classes of small molecules
2022-04-14
Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymati
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The present results indicate that
2022-04-14
The present results indicate that oxidative damage in CFS muscles is not due to the decline in the efficiency of antioxidative enzymes. This suggests that there is an increase in the generation of reactive oxygen species consistent with a mitochondrial origin of the damage. Mitochondria represent th
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Subcellular domains where Rac is active
2022-04-14
Subcellular domains where Rac is active show limited Rho activity and vice versa (Fig. 4). This distinctive patterning in Rho activity is achieved via the downstream Rac effector Par6, an important part of the so-called Par polarity complex. In primary epithelium, the cytoskeleton and associated Rho
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nrf2 inhibitor Furthermore a direct thiol protective
2022-04-14
Furthermore, a direct thiol protective role of S-nitrosylation has been reported in animals [66]. Here, formation of higher order irreversible oxidative modifications, such as sulfinic and sulfonic acids were prevented by S-nitrosylation. All these observations underline the important role of ROS in
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In this study we explore different mathematical models for
2022-04-14
In this study, we explore different mathematical models for describing the IVIVC of a preclinical dataset of 12 different dual GPR109A/GPR81 agonists. The objective is to establish a predictive model of in vivo lipolysis suppression in the rat based on in vitro potency data. First, a nonlinear mixe
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In the present study recipient oestradiol serum levels on th
2022-04-14
In the present study, recipient oestradiol serum levels on the day of donor oocyte retrieval or warming were found to be significantly higher in the antagonist group and higher than 100 pg/ml in all cases. Serum oestradiol level has been reported to have no effect on endometrial receptiveness in ooc
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br Conclusion br Conflict of interest
2022-04-14
Conclusion Conflict of interest Acknowledgments This work was supported by an NRF grant (2016R1A2B4011196) from the Korea Research Foundation. Introduction Thymic epithelial tumors are rare, but they are the most common primary neoplasm of the thymus and of the anterosuperior mediastinu
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br Materials and methods br Results br
2022-04-14
Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast Psora 4 by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs within minutes and w
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In the present study five Glu substituted analogues of GIP
2022-04-14
In the present study, five Glu3-substituted analogues of GIP, namely (Ala3)GIP, (Lys3)GIP, (Phe3)GIP, (Trp3)GIP and (Tyr3)GIP, were synthesised and tested for DPP-IV resistance and biological activity both in vitro and in vivo. The properties of these analogues were compared with native GIP and (Pro
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Various strategies have been pursued
2022-04-14
Various strategies have been pursued in the search for GIPR antagonists. Antibodies raised against both GIP(1–42) [14], [15] or the GIPR [16], [17], a small molecule antagonist [18], amino flavopiridol substitutions of GIP(1–42) [19], and various GIP(1–42) truncations and modifications such as e.g.
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br Activators Many compounds are known to influence the
2022-04-14
Activators Many compounds are known to influence the activity of Ca2+-activated K+ channels, and since hIK1 was cloned more insight has been gained on compounds that have the capacity to increase channel activity. Activation by divalent metal cations has been investigated, with Ca2+, Pb2+, Cd2+,
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Many neutral and acidophilic galactosidases have been purifi
2022-04-13
Many neutral and acidophilic β-galactosidases have been purified from microorganisms [14], while only a few alkalophilic β-galactosidases have been reported [19]. An alkalophilic β-galactosidase, BGal_375, was obtained and researched for the characterization of its hydrolytic activity. BGal_375 show
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The current gold standard for diagnosing BAM or
2022-04-13
The current gold standard for diagnosing BAM or BAD is the measurement of BA turnover rate with radiolabelled tauroselcholic (75selenium) straight from the source (also known as the SeHCAT retention test). SeHCAT test involves the use of a synthetic analogue of naturally occurring conjugated tauroch
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CC is a widespread disorder affecting up to
2022-04-13
CC is a widespread disorder affecting up to 20% of people worldwide, which also deteriorates the quality of life of patients and causes a substantial economic burden to society. There are 3 categories of CC: normal-transit constipation, slow-transit constipation and defecatory or rectal evacuation d
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