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The inhibitory activities of new
2021-10-11

The inhibitory activities of new compounds against P. aeruginosa were determined in both DTSB media supplemented with heme or free iron and LB media (Table 1). The MIC50 values of the compounds ranged from 42 to 260 μg/mL in DTSB medium and from 26 to 230 μg/mL in LB medium. Among these new inhibito
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The manuscript provides mechanistic insights into
2021-10-11

The manuscript provides mechanistic insights into the suppression of EGFR, BCRP, PKM2, and other cancer biomarkers in response to pharmacological inhibition of GPR55 with MNF and CID (Fig. 7). Firstly, inactivation of ERK has been previously demonstrated following treatment of PANC-1 needs your atte
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A subsequent modeling study by a different group was based
2021-10-11

A subsequent modeling study by a different group was based on the bovine rhodopsin homology model using the 1L9H construct [38]. However, the site-directed mutagenesis data and docking suggested that the niacin-binding pocket is different to that described in the aforementioned report, but similar t
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While NR upregulation in the spinal cord
2021-10-11

While NR1 upregulation in the spinal cord is known to contribute to pathological pain [7], [22] and furthermore, NR1 expression in the spinal cord has been shown to be reduced by continuous administration of the GlyT1-inhibitor ALX5407 [23], little is known about possible expressional changes of NR1
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Herein we report the discovery of AM AM
2021-10-11

Herein, we report the discovery of AM-3189 (). AM-3189 maintains the in vivo efficacy of AMG 837 while displaying a superior pharmacokinetic profile and minimal CNS exposure. As we reported previously, activity on the GPR40 receptor varies significantly with substitution at the β-carbon relative to
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The classical genomic effects of GR come about through ligan
2021-10-11

The classical genomic effects of GR come about through ligand-bound GR homodimerizing in the nucleus and via direct binding to GREs on the target genes, bringing about transcriptional activation or repression. Examples of target genes up-regulated by activated GR include genes encoding β2-adrenergic
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In summary PPARG and FFAR are
2021-10-09

In summary, PPARG and FFAR1 are connected in several ways, and the presented interaction is mechanistically reasonable. Additional investigations are required to elucidate the exact details of the underlying physiology. However, our findings are of immanent importance for the treatment of type 2 dia
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Although exhibited high inhibitory activity was found to be
2021-10-09

Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , and
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The feasibility of using the Fas Fas
2021-10-09

The feasibility of using the Fas/Fas ligand (FasL) system to target vascular progenitor DAPI hydrochloride contributing to intimal hyperplasia has been shown in many studies [[18], [19], [20], [21], [22], [23], [24]]. Fas receptor, a member of tissue necrosis factor family, is a death receptor that
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TNP-470 Cell stiffness is determined by
2021-10-09

Cell stiffness is determined by the cytoskeleton, an intracellular polymeric network consisting of TNP-470 filaments, microtubules, intermediate filaments, and crosslinking proteins [38]. Low cell stiffness has been correlated with reduced formation of well-defined F-actin filaments or bundles [39]
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br STAR Methods br Acknowledgments We thank
2021-10-09

STAR★Methods Acknowledgments We thank Prof. Y. Tomari at the University of Tokyo for experimental advice and K. Hanada for technical assistance. This research was supported by Grants-in-Aid for Scientific Research on Innovative Areas “Nascent Chain Biology” (JP15H01548 and JP17H05677 to T.I. a
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The vessel wall protein collagen
2021-10-09

The vessel wall protein collagen, which becomes exposed to circulating platelets after vascular injuries, is a very strong platelet agonist. It stimulates all relevant platelet activation steps predominantly via the GPVI/FcRγ-chain receptor complex through an immunoreceptor tyrosine-based activation
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Migratory properties of Treg are
2021-10-09

Migratory properties of Treg are extremely important for the potential in vivo application. Therefore, the observed expression of CXCR3 on almost all obtained insulin-specific Treg is crucial for directing WAY-100635 maleate salt into the inflamed tissue (in this case pancreatic islets). CXCR3 resp
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It is interesting to note that GlyT and GlyT
2021-10-09

It is interesting to note that GlyT1 and GlyT2 are modulated in a coordinated and opposite way as that shown in this work by different mechanisms and situations. An example is the purinergic control of GlyT1 and GlyT2 through P2Y receptors in brainstem and spinal cord neurons. This mechanism promote
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br Excitatory amino acid transporter mediated glutamate
2021-10-09

Excitatory amino apiii australia transporter-mediated glutamate transport Early studies detailing the presence of uptake systems capable of transporting glutamate and aspartate into neurons and glia represented a critical step in the overall task of demonstrating that l-glutamate was indeed an e
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