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Ulimorelin also known as TPZ is a macrocyclic molecule
2021-10-29
Ulimorelin, also known as TPZ101, is a macrocyclic molecule that is a potent agonist of the ghrelin receptor (Hoveyda et al., 2011). Due to its ability to stimulate gastrointestinal motility, ulimorelin has been evaluated as a possible treatment in gastroparesis (Ejskjaer et al., 2010), ileus (Frase
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br A small conductance chloride
2021-10-29
A small conductance chloride channel (SCC) In addition to the above-described channels, a 5pS SCC has been encountered in electrophysiological recordings. This channel, exhibiting long periods of opening separated by long intervals of closing, showed the same characteristics as the SCC described
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The atomic model of Ce INX provides an additional
2021-10-29
The atomic model of Ce-INX6 provides an additional interpretation to the Ce-INX6ΔN mutant structure at low-resolution [41]. Given that the N-terminal residues from 2 to 19 are deleted in the Ce-INX6ΔN mutant, the N-terminal funnel found in the pore of the wild-type Ce-INX6 should be lost in the Ce-I
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There are many kinds of
2021-10-29
There are many kinds of neurological disorders and neuropsychiatric diseases, like stroke, dementia, schizophrenia and so on. Among these disorders, the most important reason for choosing depression in our study is that FXR has already been demonstrated to regulate the function of CREB, which is clo
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br Conclusions and perspectives In conclusion offering duly
2021-10-29
Conclusions and perspectives In conclusion, offering duly validated and highly performing assays for measuring DiXaIs in plasma is a step, but not the final issue. More dedicated and individual assays will continue this innovative development, which witnesses the need for collaboration between co
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There are several basic science studies that aim to investig
2021-10-29
There are several basic science studies that aim to investigate potential mechanisms behind the reduced incidence of MI in factor Xa inhibitor treated patients. Perzborn et al. reported that in-vitro addition of rivaroxaban reduced tissue-factor induced platelet aggregation (Perzborn, Heitmeier, & L
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In various models histamine has been shown to induce
2021-10-29
In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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The inhibitory activities against HDAC
2021-10-28
The inhibitory activities against HDAC1 and HDAC6 of title compounds were evaluated in a fluorescent assay using SAHA and ACY-1215 as positive control. The results were displayed in A. Compounds – with linker containing 5–7 carbons showed good inhibitory activities against HDAC6. They also displayed
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br Role of dynamin in NPRA endocytosis
2021-10-28
Role of dynamin in NPRA endocytosis In recent studies using 125I-ANP binding assay and confocal microscopy, we have examined the role of dynamin in the internalization and trafficking of NPRA in a stably transfected HEK-293 PYR-41 [69]. Our findings indicated that ANP treatment of high-density NP
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br cAMP cGMP effector systems in human platelets PKA
2021-10-28
cAMP/cGMP effector systems in human platelets (PKA, PKG, PDEs) In eukaryotic cells, the effects of intracellular cAMP are mediated by two types of cAMP-dependent protein kinases (PKA type I and II) and cAMP-regulated guanine nucleotide exchange factors (EPAC/cAMP-GEF) which activate the RAS GTPas
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Indeed in women with different causes of
2021-10-28
Indeed, in women with different causes of epithelial layer damage, HIV infection rates have been reported to be very high [2], [3]. As observed from in vivo studies, disruption of the epithelium due to pathogens [45], [46] or chemical irritants [47], has resulted in women being at a higher risk of H
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Crystal structures from soluble E constructs Khan et al
2021-10-28
Crystal structures from soluble E2 constructs (Khan et al., 2014; Kong et al., 2013) have revealed globular protein with no regular structure in spite of having eight disulphide bonds (Kong et al., 2013). Although 62% of the protein exists in loops or disordered structures, overall it was well-defin
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In order to facilitate the preparation of aminothiazoles con
2021-10-28
In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to
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br Results and discussion br Conclusion In summary we
2021-10-28
Results and discussion Conclusion In summary, we designed and discovered a series of novel GPR40 agonists containing 3,5-dimethylisoxazole with improved tPSA and ideal cLog P. Most of these compounds were confirmed as excellent GPR40 agonists in vitro. Especially, compound 11k exhibited robust
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The F P concentration reported for a resting rabbit
2021-10-28
The F6-P concentration reported for a resting rabbit muscle [20] reduced the KAapp for aldolase–FBPase complex more than 50 times compared to KAapp for aldolase–FBPase in the absence of effectors (Fig. 1b and Table 1). A standard assay for determination of FBPase activity in a complex with aldolase
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