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Herein in consider of the high similarity
2021-12-20
Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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VU 0155069 A model substance often used in the studies
2021-12-20
A model substance often used in the studies of oxidative processes in erythrocytes is tert-butyl hydroperoxide (t-BHP), which, being lipophilic, passes easily across the erythrocyte membrane [9]. In erythrocytes treated with t-BHP (0.1–3mM) for less than 1h, a dramatic decline in the reduced glutath
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In summary our findings provide the evidence
2021-12-20
In summary, our findings provide the evidence and the mechanistic understanding of the protective effects of GIP receptor agonist, D-Ala2GIP, in the MPTP-induced neurotoxicity in mice. The observed protective effects are potentially due to reduced oxidative stress and attenuation of dopamine loss in
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There are multiple docking platforms suitable for
2021-12-20
There are multiple docking platforms suitable for use with nucleic dgat inhibitor receptors. These include: DOCK v4-6 (UCSF) [[68], [69], [70]], AutoDock (Scripps) [71], AutoDock Vina (Scripps) [72], GOLD (Cambridge Crystallographic Data Centre) [73], Surflex-DOCK (BioPharmics) [74], Glide (Schrӧdi
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The ability of GPX and other selenoproteins to be selectivel
2021-12-20
The ability of GPX4 and other selenoproteins to be selectively induced by ferroptotic stimuli suggests that the stress-induced increase in the transcription of a number of putative, “antioxidant” selenoproteins is an adaptive homeostatic, but insufficient response to prevent cell death in the face o
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The deduced amino acid sequences of all
2021-12-20
The deduced amino cox 2 inhibitor sequences of all scIPPSs display high similarity, and sequence alignments reveal seven conserved regions [2]. Regions II and VI contain the substrate-binding regions, with two characteristic aspartate-rich motifs (DDx(xx)xD; where x represents any amino acid residu
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Colorectal cancer CRC is the leading cause of cancer deaths
2021-12-20
Colorectal cancer (CRC) is the leading cause of cancer deaths in Taiwan and is also a most common cancer in the world (Huang et al., 2012, Jemal et al., 2011). With early detection and treatment in the initial stage, CRC can be recognized as curable in comparison with other malignant tumors (Levin e
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In an effort to more fully explore the
2021-12-20
In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold
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Accumulating evidence suggests that the NGF
2021-12-20
Accumulating evidence suggests that the NGF family of neurotrophins have important modulatory roles in opioid analgesia and addiction [36]. The NGF family of neurotrophins include NGF, PHA-793887 derived neurotrophic factor (BDNF), neurotrophin-3 (NT3), and neurotrophin-4 (NT4) [37]. BDNF knockout
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Although it is currently unknown why the longer splice
2021-12-18
Although it is currently unknown why the longer splice variant found in the human has not been found in any other species, similar results have been reported for other receptors, including the pik 2 receptor splice variant ERbeta2 identified in human and primate, but not other species (Sierens, et
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br Materials and methods br Results
2021-12-18
Materials and methods Results Conclusions We developed a glutamate biosensor with chitosan as a matrix for the immobilization of the enzyme glutamate oxidase on the surface of a platinum electrode. Our miniaturized biosensor of 50 µm in diameter can be applied for monitoring glutamate in vi
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A oligomers increased ubiquitination of GLT in astrocytes Pr
2021-12-18
Aβ1-42 oligomers increased ubiquitination of GLT-1 in astrocytes. Previous studies found that astrocytic GLT-1 is internalized from the cell surface by ubiquitination of lysines located in the cytoplasmic C-terminus of the transporter (Gonzalez-Gonzalez et al., 2008, Martinez-Villarreal et al., 2012
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The transport of glutamate by EAAT
2021-12-18
The transport of glutamate by EAAT2 from the extracellular fluid into either astrocytes or endothelial cells is an unfavorable and energy-consuming process. This energy is provided by a coupled co-transport of three sodium ions, one proton, and one glutamate molecule in the counter-transport of one
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br Acknowledgments br Introduction Postmenopausal osteoporos
2021-12-18
Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by NHS-12-Biotin synthesis deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approxi
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br Materials and methods br Results br
2021-12-18
Materials and methods Results Discussion Employment of GIPR signaling, specifically the direction of this manipulation, as a strategy to improve body weight remains a contentious subject of intense scientific investigation [22], [32], [33]. Despite the physiological benefits of GIP on BAY 5
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