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Growing evidence supporting the anti inflammatory and tissue
2022-07-16

Growing evidence supporting the anti-inflammatory and tissue-protective effects of FPR antagonists led to the screening of commercial libraries for novel small-molecule FPR antagonists. As result of these screening efforts and/or structure–activity relationship (SAR)-directed design and synthesis, a
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Altiratinib Through the analysis of various
2022-07-16

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Altiratinib motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering
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(-)-Bicuculline methobromide Focal adhesion kinase FAK also
2022-07-15

Focal adhesion kinase (FAK), also known as protein tyrosine kinase2 (PTK2), is a tyrosine kinase and vital member in integrin-mediated signaling pathways [3]. In response to integrin involvement, FAK would be phosphorylated. It was reported that FAK is involved in cellular adhesion and spreading [4]
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Collectively these observations demonstrate that FAAH is fun
2022-07-15

Collectively, these observations demonstrate that FAAH is functionally positioned to modulate the actions of AEA and other NAEs on BLA neurons and anxiety processes mediated by this region. By extension, manipulations that lead to alterations in FAAH activity, such as stress or administration of com
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summarizes FAAH inhibition data for a
2022-07-15

summarizes FAAH inhibition data for a series of 4-[2-benzofuran]2-yl-pyrimidines substituted with a pyrrolidine, piperidine or homopiperidine bearing a methyl-ketobenzimidazole unit. As indicated, the 3-(keto-benzimidazole-3-yl)piperidine displayed potent inhibition of hFAAH and moderate inhibitio
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In human cancers it has been
2022-07-15

In human cancers, it has been identified that FOXC2-AS1 functions as an oncogenic RNA. For instance, in osteosarcoma, FOXC2-AS1 regulates the expression of FOXC2 at the transcription and post-transcription levels to promote doxorubicin resistance by facilitating ABCB1 expression (C.L. Zhang et al.,
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DLS only provides a Z average
2022-07-15

DLS only provides a Z-average size based on spherical model, hence the size of nanorods was determined as 300 nm by DLS measurement. However, the size of length is nearly 400 nm while width is about 100 nm, which was clearly observed by transmission electron microscopy (TEM) (D). Meanwhile, the TEM
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The H R antagonist cimetidine
2022-07-15

The H2R antagonist cimetidine (Tagamet™) became the first billion-dollar drug in the 1980s for the treatment of peptic ulcer disease. Other H2R antagonists include ranitidine, famotidine, nizatidine, and zolantidine, the latter showing good BBB penetration with a steady-state brain/blood ratio of 1.
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Histamine functions as a key neurotransmitter in multiple ci
2022-07-15

Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, histamine is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histamine recycling pathway
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In first wave first generation drugs telaprevir and
2022-07-15

In 2013, first-wave, first-generation drugs telaprevir and boceprevir was the first protease inhibitors (PIs) incorporated in Brazilian Clinical Guidelines for the treatment of patients infected with HCV KN-92 phosphate 1. Based on this 2013 Clinical Guideline, telaprevir could be used for both naï
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DNA methylation is a kind of epigenetic modifications that
2022-07-15

DNA methylation is a kind of epigenetic modifications that can be described as a heritable alteration in gene expression, without any changes in the DNA sequence. Recent evidences suggest that the regulation of DNA methylation status is a frequent and early event in prostate carcinogenesis. For exam
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All experiments in this study were performed at pD
2022-07-15

All experiments in this study were performed at pD 6.1 for reasons described above. This leaves a question about the implications of stereochemistry in vivo. At physiological pH the GSTP1-1 catalyzed rate of EASG formation is only 1.1-fold higher than the non-enzymatic rate [26]. However, when human
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The opposite modulation observed for
2022-07-15

The opposite modulation observed for circulating LPI levels and WAT GPR55 MRS 2179 tetrasodium salt receptor by nutritional status suggests that increased levels of LPI may down-regulate the expression of its receptor in WAT, whereas in conditions of low serum LPI levels, the expression of GPR55 is
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Introduction Non alcoholic hepatic steatosis is characterize
2022-07-15

Introduction Non-alcoholic hepatic steatosis is characterized by the presence of steatosis in hepatocytes [1], which leads to the development of fatty liver [2]. It is strongly associated with obesity, insulin resistance, and type II diabetes [3]. They are major risk factors of non-alcoholic hepati
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In this review we aim to provide a comprehensive understandi
2022-07-15

In this review, we aim to provide a comprehensive understanding of: 1) how AT-resident CD4+ T cell subpopulations regulate the metabolic status of AT; and 2) how adipocytes as antigen presenting cells to modulate the activities of CD4+ T cell subpopulations in AT. Under condition with obesity, ad
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