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Kobe0065 A major hurdle in purifying a
2022-06-20

A major hurdle in purifying a membrane protein is finding a detergent that can preserve the protein, after releasing it from a given membrane, in a stable and non-aggregated state during purification steps [18,50]. The ability of various detergents used to solubilize and purify membrane proteins has
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We noticed that the spontaneous openings
2022-06-20

We noticed that the spontaneous openings of the D97R α1 GlyR appeared to be quite similar to those elicited by a maximally-effective glycine concentration on wildtype GlyR; both generated similar open and shut dwell-time histograms, both exhibited openings grouped into clusters with Popen values gre
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Next we investigated the accumulation
2022-06-20

Next, we investigated the accumulation of [3H]-ribavirin in fresh villous fragments of human placenta, which provide a physiologically relevant, well-described and validated model for assessing drug interactions with ENTs [32], [35], [69], [70]. The uptake of [3H]-ribavirin was time-dependent and si
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The precise mechanisms of action of PBA are as yet
2022-06-20

The precise mechanisms of action of 4-PBA are as yet ambiguous. Its capacity as a chemical chaperone has been thoroughly documented for the ABC transporter family in particular (Prulière-Escabasse et al., 2007; Iram and Cole, 2014; Gordo-Gilart et al., 2016; Pomozi et al., 2017). 4-PBA has been clas
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The unique mechanism of EAAT anion channel gating
2022-06-20

The unique mechanism of EAAT anion channel gating results in neuronal or glial anion conductances that follow changes in substrate concentrations and thus allow feedback control of glutamate release (Wersinger et al., 2006) or modification of GABAergic postsynaptic currents by glutamatergic signals
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Oxytocin receptor br Conclusion br Conflict of interest br A
2022-06-20

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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Extending time action is another strategy to
2022-06-18

Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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We speculated modulation of redox balance in brain by
2022-06-18

We speculated modulation of redox balance in brain, by activation of GIP receptor pathway. QA is known to mediate production of ROS, lipid peroxidation by its interactions with Fe2+ and formation of QA-Fe2+ complex (Braidy et al., 2010, Rios and Santamaria, 1991, Stipek et al., 1997). QA induces NO
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br Conclusions br Acknowledgement Work in the authors labs w
2022-06-18

Conclusions Acknowledgement Work in the authors’ labs was funded by Natural Sciences and Engineering Research Council of Canada (OGP0194652 and OGP0041653) and Diabète Québec. Introduction Fifty years ago, Sydney Brenner proposed Caenorhabditis elegans as a useful model for the study of an
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Introduction G quadruplexes are therapeutically important
2022-06-18

Introduction G-quadruplexes are therapeutically important non-canonical nucleic CAY10499 structures that are formed by a planar assembly of four guanines, termed G-tetrads (Fig. 1), in the guanine rich regions of genome [[1], [2], [3]]. As it is getting increasingly established, several life forms
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Recently Bristol Myers Squibb and Merck reported their
2022-06-18

Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic flunixin meglumine mg derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR4
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To investigate an involvement of
2022-06-18

To investigate an involvement of GPR120 and GPR40 in the enhancement of cell motile activity of MG-63 cells, highly migratory (MG63-R7) NSC23766 were established from MG-63 cells (Fig. 2A). The expression level of GPR120 gene was significantly higher in MG63-R7 cells than in MG-63 cells, while no c
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All of the abovementioned effects of
2022-06-18

All of the abovementioned effects of PUFAs signal their involvement in a cellular phenotype switching phenomenon, which is increasingly recognized as a potential target for future pharmacotherapies of atherosclerosis, especially for individuals who do not respond to the classical lipid-lowering stra
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Benzethonium Chloride A pyrimidine class of compounds is
2022-06-18

A pyrimidine class of compounds is of enormous interest within anti-HIV drug discovery process for several decades, as pyrimidine based DABOs class [7], DAPYs class [8] are well known as NNRTIs as well as NRTIs. However, the overall role of a pyrimidine class of heterocycles in anti-HIV drug discove
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The imidazopyridines and related imidazopyrimidines
2022-06-18

The imidazopyridines and related imidazopyrimidines – and – were constructed from the key amine intermediates – ( X=CH and Ar=2-FPh, X=N and Ar=2-FPh, X=CH and Ar=5-pyrimidine, X=CH and Ar=2-methyl-5-pyrimidine, and X=CF and Ar=2-methyl-5-pyrimidine). These were synthesized a modified Horner–Em
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