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Taken together BRP represents a
2024-06-06

Taken together, BRP-187 represents a novel chemotype of LT biosynthesis inhibitors with outstanding potency in human PMNL and monocytes activated under pathophysiological relevant conditions and with effectiveness in vivo. Using the PLA that visualizes the in situ interaction between 5-LO and FLAP i
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The present study showed for
2024-06-06

The present study showed, for the first time, that hirsutine, hirsuteine, rhynchophylline, isorhynchophylline, corynoxeine, and isocorynoxeine in yokukansan can inhibit the 5-HT3 receptor current. These data indicate that part of the effect of yokukansan against the behavioral and psychological symp
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A contribution of V ATPase subunits specifically to phagosom
2024-06-05

A contribution of V-ATPase subunits specifically to phagosome-lysosome fusion was uncovered by Peri and Nüsslein-Volhard who described that depletion of the VO subunit a1 in zebrafish interferes with phagosome maturation in microglial 4-DAMP (Peri and Nusslein-Volhard, 2008). However, loss of the V
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The Type A series contains
2024-06-05

The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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Introduction Initially postulated to represent the
2024-06-05

Introduction Initially postulated to represent the main source of ATP production in eukaryotic cells, mitochondria are recently recognized to perform manifold essential functions beyond energy production, impacting most areas of cell biology and medicine [1]. Mitochondrial metabolism is both the ba
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The mitochondrial protein AIF was the first caspase independ
2024-06-05

The mitochondrial protein AIF was the first caspase-independent death effector. AIF can induce caspase-independent chromatin condensation and large-scale DNA fragmentation to approximately 50 KB. AIF that is released to cytoplasm can mediate apoptosis when special extracellular signals trigger the o
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br Conclusions br Acknowledgements We would like
2024-06-05

Conclusions Acknowledgements We would like to thank the members of the Bergmann lab for fruitful discussions in the course of this work. This work was supported by the National Institute of General Medical Sciences (NIGMS) under award number R35 GM118330. The content is solely the responsibili
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br Experimental section br Acknowledgment S B
2024-06-05

Experimental section Acknowledgment S.B.T. is grateful to the Deutsche Forschungsgemeinschaft (DFG), the Wilhelm Sander-Stiftung and Interdisciplinary Center for Molecular Materials (ICMM) for generous research support. M.M. greatly acknowledges the experimental support and the scientific cont
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Growth inhibition assays are the
2024-06-05

Growth-inhibition assays are the most commonly used to identify antifungal small molecules. However, they have several facts that limit their use since many pathogenic fungi grow as filaments making difficult a correlation between growth and OD (optical density). They are not useful for identifying
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br G protein activation through croaker ZIP An essential cri
2024-06-05

G protein activation through croaker ZIP9 An essential criterion for designating a steroid binding protein as a membrane steroid receptor is to demonstrate that it can transduce steroid signals in order to elicit a cellular response. Treatment with 100nMT caused G protein activation in croaker ZI
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N terminally extended antigenic peptide precursors that surv
2024-06-05

N-terminally extended antigenic peptide precursors that survive cytosolic degradation and enter the ER, need to be further processed by ERAP1 and/or ERAP2, in order to acquire the right length required for MHCI binding. ERAP1 (ERAAP in mouse) is an IFN-γ-inducible, metalloaminopeptidase that trims N
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In this study Rb increased the phosphorylation of p
2024-06-05

In this study, Rb1 increased the phosphorylation of p38 MAPK and Akt and macrophage phagocytosis of bacteria in mouse lung cells, consistent with the in vitro results. A recent study showed that Rb1 diminished the severity of lung injury in rats exposed to LPS. Rb1 inhibited the LPS-induced increase
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In addition we aimed to examine the possible role
2024-06-05

In addition, we aimed to examine the possible role of adiponectin in modulating changes in IR. It was observed that there was a simultaneous decline in expression of IR and AdipoR1 proteins in the ovary of PCOS-mice as compared to the control ovary. Further, a strong correlation was found between ch
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br Conclusion In this brief
2024-06-04

Conclusion In this brief Letter, we report an easy method for the preparation of the antileukemic natural product 1. Using a biomimetic strategy,1, 8 in which the aromatic residues are attached to a lysine moiety prior to the reduction of the central carboxylate group, a step-economical synthesis
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IC values were obtained for an
2024-06-04

IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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