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The replacement of the P butyl urea cap with
2022-03-26

The replacement of the P-butyl urea cap with sulfonamide derived cap had a profound effect on binding. Compound obtained by the replacement of -butyl urea P cap of compound with sulfonamide demonstrated a =34nM, a fifteen folds improvement in potency. Similarly replacement of P-butyl cap in the P cy
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We observed that the Toc G domain recognizes the N
2022-03-26

We observed that the Toc159G domain recognizes the N-terminal portion of the transit peptide of pSSU with a dissociation constant of 70 μM (Fig. 2; Table 1), while a tenfold higher KD was obtained for the phosphorylated C-terminal region. In turn, the homodimer of Toc34G recognizes the phosphorylate
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br GSK Glycogen synthase kinase GSK
2022-03-25

GSK-3 Glycogen synthase kinase-3 (GSK-3) is a ubiquitous serine/threonine kinase that is involved in multiple signaling pathways that are crucial for cellular metabolism and proliferation (Doble and Woodgett, 2003, Frame and Cohen, 2001, Grimes and Jope, 2001, Woodgett, 1990). GSK-3 is known to d
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br Materials and methods br Results
2022-03-25

Materials and methods Results Discussion Main results obtained in this work are presented in Table 1 and can be summarized as follows: 1) AEA inhibits FcεRI receptor-induced degranulation with the participation of CB2 and GPR55 receptors by a PTX-insensitive mechanism; 2) AEA does not block
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Excessive adiposity is also a key pathogenic factor in the
2022-03-25

Excessive adiposity is also a key pathogenic factor in the development of CVD. Through reductions in bodyweight, GPR120 agonism is therefore also implicated as a potential therapy for obesity and heart and vessel disease. In addition to weight loss, when compared with their wild-type littermates, GP
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The synthesis of nitropyrimidine analogs was outlined in Dic
2022-03-25

The synthesis of 5-nitropyrimidine analogs – was outlined in . 4,6-Dichloro-5-nitropyrimidine, 4-methylsulfonylaniline and 2-fluoro-4-methylsulfonylaniline were prepared according to previously reported procedures., , Reaction of 4,6-dichloro-5-nitropyrimidine and substituted aniline in DMF yielded
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In this study we provide biochemical and immunohistochemical
2022-03-25

In this study we provide biochemical and immunohistochemical evidence for the localization of the glycine transporter GLYT1 in synaptic vesicles. Previously, it was thought that GLYT1 was exclusively a glial protein (Zafra et al., 1995a). However, due to a partial discrepancy between mRNA and protei
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A major hurdle in purifying a membrane protein is
2022-03-25

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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br Perspectives br Contributors BP study concept design
2022-03-25

Perspectives Contributors BP: study concept & design, literature review, data analysis & synthesis & presentation, primary draft of the manuscript; JDR: data analysis, Fig. 1 illustration, manuscript review & revision; ZP: study concept & design, manuscript review & edit; MI: manuscript review
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terbinafine hydrochloride The neuronal glycine receptor HSOR
2022-03-25

The neuronal glycine receptor/3α-HSOR/allopregnanolone pathway may also be extended to the central nervous effects of gelsemine and koumine in brain. 3α-HSOR is expressed in certain brain regions in rats and humans, such as the limbic system including hypothalamus, hippocampus and amygdala, in addit
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Throughout the last few decades evidence has accumulated ind
2022-03-25

Throughout the last few decades, evidence has accumulated indicating that NTTs, whose primary location is the cell surface, are subject to a series of regulatory processes of intracellular traffic to and from the membrane (Robinson and Jackson, 2016; Vaughan and Foster, 2013). In addition, lateral m
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Although most of the incretin
2022-03-25

Although most of the incretin effects on ion channels metabolism can be secondary to their action on insulin/glucagon secretion, some evidence strongly suggests that they could also act directly on liver glucose utilization and production [4], [13], [22], [27], [34], [44]. Supporting this concept,
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The glucocorticoid GR complex exerts wide spread cellular ef
2022-03-25

The glucocorticoid-GR complex exerts wide-spread cellular effects through two distinct mechanisms categorized as genomic and non-genomic pathways [3,39]. Most non-genomic pathways originate from activation of mGR [40]. These actions of the GR appear to all play an important role in the regulation of
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br Acknowledgments We would like
2022-03-25

Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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br Acknowledgments br Introduction When human red blood cell
2022-03-25

Acknowledgments Introduction When human red blood cell (hRBC) membranes are depolarized, either as intact dextromethorphan hydrobromide suspended in depolarizing (low Cl−) Ringers or under voltage clamp conditions using excised inside-out patches, they respond by opening a nonselective voltag
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