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br Membrane Fusion Requires Rab GTPases Tethers and SNAREs
2022-03-18
Membrane Fusion Requires Rab-GTPases, Tethers, and SNAREs Regulation and Function of Rab5 Following endocytosis in metazoan cells, the Rab5-specific GEF Rabex5 binds to ubiquitinated cargo proteins, such as cell surface receptors or metabolite transporters, and subsequently activates Rab5 on e
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In order to investigate whether this off target activity was
2022-03-18
In order to investigate whether this off-target activity was related to a particular structural feature of this NLG-8189 or was characteristic of the series, compounds , and were selected as being matched pairs with compound but with structural variation in terms of the R, R and R groups, respective
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In summary through medicinal chemistry design and
2022-03-18
In summary, through medicinal chemistry design and computer-assisted conformational modeling, the initial lead was evolved into a series of dihydrobenzofuran derivatives, , as potent GPR119 agonists. Optimization of general structure at various regions of the molecule, including the substituent on d
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Here we demonstrate an anti inflammatory and anticancer
2022-03-18
Here we demonstrate an anti-inflammatory and anticancer function for Gpr109a in colon. Gpr109a signaling imposed anti-inflammatory properties in colonic antigen-presenting cells, which in turn induced differentiation of Treg cmv virus and IL-10-producing T cells. Gpr109a was also required for the e
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The general synthetic routes leading to aspartate and diamin
2022-03-18
The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic Cy5.5 hydrazide analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid. It is worth mentio
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Tetrazole is one of the most
2022-03-18
1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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just like With the advent of genome sequencing
2022-03-17
With the advent of genome sequencing, hexokinase gene sequences are now available from a far greater number of vertebrate species, as well as from diverse non-vertebrate animal species. As indicated above, searches of vertebrate genome sequences revealed the existence of a novel fifth member of the
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Yeast two hybrid screening studies have provided the foundat
2022-03-17
Yeast two-hybrid screening studies have provided the foundation for countless investigations of protein-protein interactions [[141], [142], [143]]. To identify additional hepatic proteins similar to GKRP that are implicated in GCK regulation, a group of researchers conducted a two-hybrid study using
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Importantly the levels of the pro
2022-03-17
Importantly, the levels of the pro-inflammatory cytokines TNF-α and IL-1β and Nf-κB, a key transcription factor in chronic inflammatory responses that is activated by pro-inflammatory cytokines, were also reduced by the drugs, confirming our previous results that demonstrated anti-inflammatory effec
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The general aim of our
2022-03-17
The general aim of our in vitro experiments was to analyze the patterns of ghrelin and GHSR-1a expression in the mammary glands of dairy goats during pregnancy and to examine the direct effect of ghrelin on cell proliferation in cultured MECs of pregnant dairy goats. For this purpose, we cultured go
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The experiments indicate that a major
2022-03-17
The experiments indicate that a major component of the vasodilatation is due to antagonism of α 1-adrenoceptors. Evidence for α1-adrenoceptor antagonism is that vasodilatation was observed in T7 High Yield Cy5 RNA sale preconstricted with α1-adrenoceptor agonists, phenylephrine or methoxamine, but
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In the course of our ongoing
2022-03-17
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric jak stat inhibitor type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise t
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Based on this evidence future research should be directed
2022-03-17
Based on this evidence, future research should be directed towards the identification of actual receptor oligomeric states at the analyzed cellular surfaces. The macromolecular organization of these oligomeric receptors might establish informational hubs, which relay ligand/receptor interactions in
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Canonical and non canonical Wnt signaling pathways play esse
2022-03-17
Canonical and non-canonical Wnt signaling pathways play essential roles in various cellular activities, including cell fate determination, proliferation, migration and gene expression [57]. The canonical Wnt pathway (β-catenin dependent pathway), is activated by the binding of Wnt ligands, leading t
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br Introduction The brain contains abundant
2022-03-17
Introduction The brain contains abundant fatty acids, which serve as constituents of membranes and as an energy source. In addition, fatty acids and their metabolites contribute to signal transduction between neurons or neurons and glial cells, suggesting that fatty acids play a crucial role in d
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