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At present drugs that specifically inhibit YAP activity are
2024-09-24

At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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Having taken a step back from affinity to gain better
2024-09-24

Having taken a step back from affinity to gain better exposure and solubility, we started work to replace the unstable oxazolinone, and address the selectivity over the hERG channel. Keeping in mind the binding mode of the series from crystal structures, triazole was identified as another mildly aci
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While the yeasts and see Glossary each contain
2024-09-24

While the yeasts and (see Glossary) each contain only one Aurora homolog, Ipl1p (increase in ploidy 1) and Ark1 (Aurora-related kinase 1), respectively 5, 6, , and Xenopus laevis contain two Aurora kinases: Aurora A and Aurora B [4]. Mammals have three Aurora kinases, A, B, and C (Figure 1). In anim
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Purification of Rv c In order to investigate
2024-09-24

Purification of Rv2477c. In order to investigate the catalytic capabilities of Rv2477c, we expressed the protein as an N-terminal histidine-tagged fusion protein in E. coli BL21 cells and purified the protein by cobalt-affinity chromatography. As shown in Fig. 2A, the 65 kDa fusion protein was expre
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br Mechanisms of homeostasis At face
2024-09-24

Mechanisms of homeostasis At face value, homeostatic mechanisms may seem like nothing more than a simple balance between opposing forces; however, the ability of Mec1/Tel1 to each orchestrate both negative and positive regulation greatly complicates the system under consideration and argues again
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Oocytes from the African clawed frog Xenopus laevis
2024-09-24

Oocytes from the African clawed frog Xenopus laevis have been widely used as an expression system to study the modulation of NMDA receptors by metabotropic receptors, such as metabotropic glutamate receptors [12], μ opioid receptors [13], insulin receptors [14] and serotonin receptors [15]. No data
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br Introduction Endothelial progenitor cells EPCs present a
2024-09-24

Introduction Endothelial progenitor cells (EPCs) present a class of blood cells with an ability to form new blood vessels relying on pre-existing vessels, which contribute to postnatal angiogenesis [1], [2]. A wide range of studies have demonstrated that EPCs play a critical role in angiogenesis
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br Results br Discussion br STAR Methods br Author
2024-09-24

Results Discussion STAR★Methods Author Contributions Acknowledgments We thank Angela Walker for assistance with the manuscript; Junlin Liu, Xiangxiang Gu, Na Chen, Lu Xue, and the BV Core Facility of iHuman Institute for their support; scientists and colleagues at Amgen Inc., Zhulun W
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The crucial role of AP in establishing and maintaining cell
2024-09-24

The crucial role of AP-1 in establishing and maintaining cell type-specific gene expression programs and cell identity is further apparent during reprogramming of mouse embryo fibroblasts (MEFs) into iPSCs with either Oct4/Sox2/Klf4/cMyc (OSKM ) factors , or chemicals . Using ATAC-seq to profile ch
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Although the earlier studies focused on the antioxidant capa
2024-09-24

Although the earlier studies focused on the antioxidant capacity of tocopherols, ascorbic 6206 and carotenoids, then it was noticed that phenolic compounds were more powerful than others (Rice-Evans, Miller, & Paganga, 1996). Phenolic compounds, the most numerous and ubiquitous groups of plant seco
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Inflammatory factors released by activated cells
2024-09-24

Inflammatory factors released by activated cells during AD are very important for the disease progression. Not only several inflammatory cytokines, such as IL-1β, IL-18, and IL-33, but also anti-inflammatory ones, as IL-10 and IL-13, are upregulated in the brain of AD patients (Morimoto et al., 2011
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HT modulates cortical and hippocampal pyramidal
2024-09-23

5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal GSK1016790A as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al.,
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As an alternative to chronic receptor blockade we have
2024-09-23

As an alternative to chronic receptor blockade, we have been targeting adenosine kinase (ADK) – an astrocyte-based enzyme that catalyses the phosphorylation of adenosine, as a means to modify 3X FLAG Peptide adenosinergic signalling (Boison, 2006, Etherington et al., 2009). Up-regulating ADK facili
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MMP-2 Inhibitor I sale Systematic administration of ABT amin
2024-09-23

Systematic administration of ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl) pyrido[2,3-d] pyrimidine), a potent and selective non-nucleoside AK inhibitor, also generates analgesic effects in animal models of pain (Jarvis et al., 2000, Kowaluk et al., 2000, Suzuki et al., 2001), sug
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br Perspectives Given the complexity of the
2024-09-23

Perspectives Given the complexity of the cellular interactome and of protein scaffolding, further progress in revealing how individual membrane proteins, including APP and AChE, interact with each other at various levels, from cell-surface shedding to gene regulation, will clarify some intrinsic
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