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Sperm exocytosis or acrosome reaction AR is
2022-06-16
Sperm exocytosis or acrosome reaction (AR) is a regulated secretion with special characteristics essential for fertilization. The AR relies on the same highly conserved molecules that drive intracellular membrane fusion and exocytosis in all other 5-Methyl-UTP (see [59] for a recent review). Two suc
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TRRAP participates in embryonic development
2022-06-16
TRRAP participates in embryonic development, as demonstrated by its binding with proteins regulating the Notch signaling pathway in fruit fly, the Ras signaling pathway in C. elegans, or the Wnt signaling pathway in 293T cells. Therefore we suspect that TRRAP variants, more especially those falling
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An isoflavone type secondary metabolite Glabrescione B GlaB
2022-06-16
An isoflavone type secondary metabolite, Glabrescione B (GlaB), from Derris glabrescens (Benth.) J.F. Macbr. from the family Fabaceae, was found to possess the capacity to bind the Gli1 zinc finger domain and to further block DNA binding capacity [118]. Pyrvinium, an anthelmintic drug approved by th
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For the SAR study human haspin kinase inhibitory
2022-06-16
For the SAR study, human haspin kinase inhibitory activity of the various compounds was evaluated using the same assay utilized for the HTS, except in the presence of varying test compound concentrations. DYRK2 kinase inhibitory activity was measured by P-incorporation into Woodtide peptide substrat
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br Consequence physiological function of ROS dependent inhib
2022-06-16
Consequence/physiological function of ROS-dependent inhibition of GSNOR Plants response to environmental changes induced by abiotic and biotic factors by enhanced accumulation of ROS resulting in temporary imbalance of the cellular redox homeostasis. This as oxidative stress/burst termed event tr
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GPR belongs to the G protein coupled receptor family
2022-06-16
GPR84 belongs to the G protein-coupled receptor family, and it was first identified from human peripheral blood neutrophils [,]. GPR84 is now considered to be a member of receptor for medium chain fatty chemokine receptor antagonist (MCFA) with carbon chain lengths of 9–14 []. GPR84 is mainly expre
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Notably Cu labeled dimeric exendin subunit which was
2022-06-16
Notably, 64Cu-labeled dimeric exendin-4 subunit, which was designated as 64Cu-Mal2Sar-(exendin-4)2, showed higher tumor uptake than that of the monomeric exendin-4 subunit [245]. Besides the most commonly-used GLP-1R agonists exendin-3 and -4 and their derivatives, exendin (9-39) exhibits strong bin
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To gain insights for further improvement
2022-06-16
To gain insights for further improvement of the agonistic activity, we compared the structural features of the -carbamate piperidine moiety in with that of the spirocyclic moiety in –. Obviously, the substituent corresponding to an isopropyl group on the -carbamate in was lacking in the spirocyclic
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Currently ursodeoxycholic acid UDCA is the only recommended
2022-06-16
Currently, ursodeoxycholic motilin receptor (UDCA) is the only recommended and widely used drug in the treatment of CFLD. However, the clinical efficacy of UDCA is controversial. The most recent Cochrane review only identified a small number of trials assessing the effectiveness of UDCA [92]. The a
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Following activation it is necessary
2022-06-16
Following activation, it is necessary for a subset of activated effector T cells to survive as long-lived memory T cells. Metabolically, this transition is dependent upon the ability of the cell to downregulate aerobic glycolysis and transition back to a more oxidative phenotype. In fact, enhancemen
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The mechanisms by which NEIL and NEIL excise bulky
2022-06-16
The mechanisms by which NEIL1 and NEIL3 excise bulky adducts and unhook ICLs are unclear. Structures of NEIL1 are available only in complex with DNA containing small lesions 79., 80., 81., and the single available structure of NEIL3 lacks DNA (Figure 5D,E) [73]. Nonetheless, comparison of the two st
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Conformational changes are observed in the LBDs
2022-06-16
Conformational changes are observed in the LBDs after ligand binding, including partial cleft closure for GluN2A and complete cleft closure for GluN1. For GluN2A, additional conformational rearrangements in the protein and ligand may be required before the ligand can be accommodated within lobe 2. F
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br Conflict of interest br Funding br
2022-06-16
Conflict of interest Funding Acknowledgements Introduction to SLC6 transporters The solute carrier (SLC) 6 family of membrane proteins perform the Na+-coupled symport of amino acids and amino rotenone derivatives into cells throughout the body. Disrupting neurotransmitter SLC6-mediated t
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Studies dealing with the effects of ischemia on
2022-06-16
Studies dealing with the effects of ischemia on EAATs have been previously reported, but some discrepancies in literature appear between them probably as a consequence of the different models, species, time of reperfusion after ischemia and age of the animals. Thus, in human, TCS 2002 stroke-depende
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In addition to the increase
2022-06-16
In addition to the increase of extracellular glutamate, ICH can also increase the levels of reactive oxygen species (ROS) and oxidative stress. Although the products of red blood cell lysis and plasma components, as well as the excitotoxic effect of glutamate have been to increase oxidative damage (
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