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The above inferences concluded that
2022-01-24
The above inferences concluded that histidine is enhancing the overall stability and rigidity of the protein which further might be restraining the protein during the transition from inactive to active state and vice-versa present in the SANT domain. Since the SANT domain binds with histone via elec
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br Author contributions br Declaration of
2022-01-24
Author contributions Declaration of conflict of interest Acknowledgements We are grateful to the Director, National Institute of Immunology for his support. The work was partially supported by J.C. Bose Fellowship to SSM. We acknowledge the help from staff of Small Animal Facility of Nation
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br Resistance to targeted therapy The
2022-01-24
Resistance to targeted therapy The idea of treating HER2 mutant tumors with specific therapies is relatively new and, as a consequence, little is known about the potential mechanisms of resistance to anti-HER2 agents in this setting. Primary resistance may be mediated by the presence of on-target
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The inhibitory concentration of atrial natriuretic
2022-01-24
The 50% inhibitory concentration of atrial natriuretic factor at midgestation and term are –7.4 ± 0.12 and –7.38 ± 0.11, respectively, demonstrating no gestational age dependency in the effect of atrial natriuretic factor on spontaneous contractile activity. Diethyl amine/nitric oxide starts to inh
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Estradiol valerate synthesis Active compounds and were furth
2022-01-21
Active compounds , , and were further tested and EC and pEC values were determined as shown in . Compound showed EC of 0.97μM (pEC 6.01) with 84.5% maximal response, which suggests that introduction of alkyl chain on aromatic nucleus of , resulted in improved GPR40 agonistic activity than that of (E
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br Materials and methods br
2022-01-21
Materials and methods Results Discussion In nerve terminals, Na+-dependent glutamate transporters of the plasma membrane are responsible for the maintenance of low (non-toxic) extracellular glutamate concentrations and accomplish uptake of glutamate into the toremifene of neurons and glial
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EAATs can transport glutamate aspartate cysteic acid and
2022-01-21
EAATs can transport glutamate, aspartate, cysteic acid, and serine-o-sulfate (Bjorn-Yoshimoto and Underhill, 2016). All EAATs work as symporters co-transporting 2 or 3 molecules of Na+ and a proton with each molecule of glutamate (or aspartate). In addition, a K+ ion is counter-transported ending in
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dpat Herein we describe the design and optimization of
2022-01-21
Herein, we describe the design and optimization of fused-ring phenyl propanoic acids as novel GPR40 agonists, leading to the discovery of compound 40a which exhibits excellent pharmacokinetic properties, improved hepatobiliary transporter inhibition, and significant glucose-lowering efficacy during
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At the heart of ferroptosis is a process of
2022-01-21
At the heart of ferroptosis is a process of lethal lipid peroxidation, which is the oxidative addition of molecular oxygen (O2) to lipids, such as polyunsaturated fatty acyl tails in phospholipids. The first descriptions of such enzymatic reactions were in 1955 by Peterson and colleagues [50] and Ro
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Cell stiffness is determined by the cytoskeleton an intracel
2022-01-21
Cell stiffness is determined by the cytoskeleton, an intracellular polymeric network consisting of Resiniferatoxin filaments, microtubules, intermediate filaments, and crosslinking proteins [38]. Low cell stiffness has been correlated with reduced formation of well-defined F-actin filaments or bundl
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br Materials and methods br Results br Conclusions In
2022-01-21
Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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Compound a substituted phenyl H pyrano
2022-01-21
Compound 6, a 5-(4-substituted-phenyl)-5H-pyrano[2,3-d:-6,5-d′]dipyrimidine derivative was invented previously to have significant efficacy to inhibit HIV integrase enzyme with 0.9 ± 0.4 μM of IC50 against 3′-processing and 16.1 ± 10.7 μM of IC50 against strand transfer suppression. The compound ind
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Interest in the non coding
2022-01-21
Interest in the non-coding genome has recently surfaced with accelerated emphasis in the past few years (Li et al., 2016). Transcription factors (TFs) bind to enhancers and mediate RNA initiation from distal transcriptional start sites (TSS) of genes. Epigenome sequencing of human and mouse during
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Now recall that a cozero element of a frame
2022-01-21
Now recall that a cozero AMG-458 of a frame L is an element of the form for some continuous real-valued function h in L. Equivalently, is a cozero element if and only if there exists an such that and . This is the pointfree counterpart to the notion of a cozero set for ordinary continuous real-v
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Several lines of evidence suggest that thermosensation in AF
2022-01-21
Several lines of evidence suggest that thermosensation in AFD is unlikely to be mediated by thermosensitive ion channels. AFD exhibits a steep temperature dependence with a reported Q of >1015 for temperature-evoked current, implying a strong amplification step in the thermotransduction process (Ram
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