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PKC s effect on quantal size may
2022-01-19
PKC’s effect on quantal size may involve regulation of endocytotic protein components responsible for mediating kiss-and-run exocytosis. There is a growing body of evidence to suggest that canonical endocytotic proteins—dynamin, amphiphysin, syndapin, and others—may play a role in modulating fusion
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Antigen presentation of incoming viral particles has been we
2022-01-19
Antigen presentation of incoming viral particles has been well studied for diverse viruses in antigen-presenting cells (APCs), mostly in dendritic cells and macrophages in the context of the exogenous antigens’ pathway to prime the CD8+ T cells. However, CD4+ T cells are not known as efficient APCs,
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The repurposing of well characterized and well tolerated dru
2022-01-18
The repurposing of well-characterized and well-tolerated drugs in order to treat illnesses for which they were not originally intended has emerged as an attractive alternative to a long and costly process of drug development. Repositioning antihistaminergic ligands seems a promising idea given that
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Whilst it has long been appreciated that
2022-01-18
Whilst it has long been appreciated that Rho-family GTPases are able to signal directly to focal adhesions, it is also becoming increasingly clear that they can achieve this indirectly, through their influence on the extracellular matrix to which the integrins bind. Cdc42 and RhoA have long been kno
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br Ketone body metabolism and neuronal excitability One
2022-01-18
Ketone body metabolism and neuronal excitability One of the best examples of the close connection between metabolism and neuronal excitability is illustrated by the effect of ketone bodies on epileptic seizures. One third of patients suffering from epileptic seizures do not respond to convention
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Recently an increasing number of studies
2022-01-18
Recently, an increasing number of studies have highlighted the crucial role of nociceptive factors produced by microglia under neuropathic pain conditions (Mika et al., 2013; Popiolek-Barczyk and Mika, 2016). iNOS is an important pronociceptive factor that is strictly expressed by microglia/macropha
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Our last area of exploration was the piperidine
2022-01-18
Our last area of exploration was the piperidine core as shown in . We rationalised that the basicity of the nitrogen (measured p=7.0) may be responsible for the affinity for the hERG receptor and we therefore sought to moderate this by incorporation of electronegative groups at the 3-position. To th
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It has been found that WHI P a JAK
2022-01-18
It has been found that WHI-P131, a JAK3 inhibitor, induced apoptosis of CD4+ T (±)-CPSI 1306 synthesis (Cetkovic-Cvrlje et al., 2012). Also, other JAK3 inhibitors (AG490 and WHI-P154) caused apoptosis in anaplastic large cell lymphoma (Amin et al., 2003). Taking into account the proapoptotic action
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A high throughput screening campaign of
2022-01-18
A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also co
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Sepsis was defined as a systemic inflammatory response
2022-01-18
Sepsis was defined as a systemic inflammatory response syndrome (SIRS) associated with severe infection in 1992 [9]. However, in the Third International Consensus Definitions for Sepsis and Septic Shock [10], it was redefined as life-threatening organ dysfunction provoked by a dysregulated host resp
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rad51 inhibitor br Author contribution br Declaration of int
2022-01-18
Author contribution Declaration of interest Acknowledgements This work was supported by National Natural Science Foundation of China (Grants 81473093) and State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica (SIMM1601ZZ-02). Introduction Diabetes represents a majo
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Pyrogallol is an organic gallic
2022-01-18
Pyrogallol is an organic gallic acid-converting compound that has three hydroxyl groups and belongs to the phenol family. Gallic Imiloxan hydrochloride is obtainable from the galls and barks of various trees, and a simple heating procedure can induce the decarboxylation of gallic acid to produce py
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PNU 37883 hydrochloride br Acknowledgments The authors would
2022-01-18
Acknowledgments The authors would like to thank principal investigator Edward John Pratt, MD (Lilly-NUS Centre for Clinical Pharmacology, Singapore) and study investigator Martha Hernandez-Illas MD (QPS-MRA) along with site staff, and trial participants and their families. We thank Zvonko Milicev
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The role of cell to cell interactions in
2022-01-18
The role of cell-to-cell interactions in coordinating the cells’ behaviour to ensure an appropriate anterior pituitary hormone response is receiving increasing attention. Anterior pituitary cyp450 inhibitors interact with neighbouring cells through junctional complexes. As their name implies, the c
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On the other hand histone deacetylase inhibitors can
2022-01-18
On the other hand, histone deacetylase inhibitors can accelerate inflammation resolution by promoting the externalization of AnxA1, a main ALX/FPR2 agonist, with concomitant inhibition of cytokine gene expression in mouse macrophages [30]. Thus, our present results provide an additional mechanism, i
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