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Other membrane currents are affected as
2020-12-24

Other membrane currents are affected as well. Some studies have provided evidence that sulfonylureas, in addition to blocking KATP channels, also inhibit chloride and calcium channels. GLYB has been shown to almost inhibit the current generated by Na+–K+ pumps in a concentration-dependent manner (wi
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br Results br Discussion The nitric oxide cyclic guanosine m
2020-12-24

Results Discussion The nitric oxide-cyclic guanosine monophosphate pathway plays an important role in normal EF, and oral PDE-5Is were developed in the late 90s after the discovery that ED occurs when there is a problem with this pathway. Since then, several PDF-5Is with different pharmacokine
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Thus the understanding of the various mechanisms
2020-12-24

Thus, the understanding of the various mechanisms of action of estrogen and SERMs is an important medical challenge and could help to develop an “ideal” SERM, preserving the beneficial effects of estrogen in the bone and urogenital system, and reducing the unwanted side effects, mainly increased ris
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br Conclusions ERK and its phosphorylation plays
2020-12-24

Conclusions ERK 1/2 and its phosphorylation plays an essential role in the hippocampus and can be triggered by both ROS accumulation and excessive Ca2+. DBP exposure can also affect the production of ROS and Ca2+ in the hippocampus. The question therefore arises as to whether the cell injury or a
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br Non cyclic nucleotide EPAC regulators Despite the success
2020-12-24

Non-cyclic nucleotide EPAC regulators Despite the success of 007 as a tool molecule, few studies to date have led to the identification of further EPAC-selective agonists. The most studied and controversial group of small-molecule EPAC regulators are the sulfonylurea (SU) family. SUs (Table 1) su
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br Results br Discussion In this paper
2020-12-24

Results Discussion In this paper we present insights into the observed specificities of inhibitors targeting the ubiquitin-activating and related E1 Triptolide via crystal structures of the specific NEDD8-E1 inhibitor MLN4924, the dual NEDD8/Ub E1 inhibitor ABPA3, and the selective Ub-E1 inhi
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Upon assembly of HLA tetramers loaded with either
2020-12-24

Upon assembly of HLA tetramers loaded with either of the two peptide versions, we could query the T cell repertoires of RA subjects and healthy individuals for the presence of cognate T cyp3a inhibitors recognizing the respective peptide-HLA complexes. We found no significant difference in frequenci
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Both receptors belong to the large family of
2020-12-24

Both receptors belong to the large family of G protein-coupled receptors (GPCRs) [4,5], which often appeared as monomers, dimers and higher order aggregates [6,7]. There is evidence that these receptor-complexes can modulate the functionality and the pharmacology of the receptors [8,9] by sequesteri
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Inappropriate heme metabolism has been linked to several neu
2020-12-24

Inappropriate heme metabolism has been linked to several neuropsychiatric disorders. In the hippocampi of Alzheimer's disease (AD) patients, for example, heme was found to binds intracellular amyloid β (Aβ), resulting in reduced heme bioavailability and its functional deficiency (Atamna and Frey, 20
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The purpose of this study
2020-12-24

The purpose of this study is to investigate KDM1B expression and its functional significance in PC. We used lentivirus-mediated shRNA to down-regulate KDM1B expression in PC cell lines in vitro and detected the changes of cell proliferation and apoptosis. These studies provided a novel insight into
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EBI remains an orphan GPCR and
2020-12-24

EBI2 remains an orphan GPCR and the identity and source of its ligand are yet to be described. Molecular studies of EBI2 have suggested that this receptor has constitutive activity, similar to that observed for many herpesvirus-encoded 7TM receptors (Benned-Jensen and Rosenkilde, 2008, Rosenkilde et
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Both the kK and kK
2020-12-24

Both, the kK3 and kK5-mediated ubiquitination leads to rapid internalisation of target proteins followed by lysosomal degradation, similar to that seen for MARCH-1/8 [77]. Ubiquitination activity of kK3 and kK5 depends on the positioning of the targeted lysine (or cysteine) residues [22]. The positi
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br Materials and Methods br Acknowledgements br
2020-12-23

Materials and Methods Acknowledgements Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the int
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We report here that DAPK signaling pathways play significant
2020-12-23

We report here that DAPK signaling pathways play significant roles in OGD-induced neuronal death. Exposure of the Diphenyleneiodonium chloride to OGD led to DAPK activation, which then promoted cell death through BimEL overexpression. Furthermore, DAPK-induced BimEL overexpression was mediated by i
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mass of cl br Transparency document br Acknowledgments
2020-12-23

Transparency document Acknowledgments This work was supported by the Ministry of Education, Youth and Sports of the Czech Republic (the National Program of Sustainability I, Grants LO1204 and LO1304), by the Czech Science Foundation (15-17282Y) and by Palacký University Olomouc (IGA_PrF_2017_0
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