A novel chrysin thiazole derivative polarizes macrophages to an M1 phenotype via targeting TLR4

Feng, Xiujing; Yu, Wenpeng; Cao, Lingsen; Meng, Fanda; Cong, Menglin

doi:10.1016/j.intimp.2020.106986

Cited by 10 publications

(6 citation statements)

References 52 publications

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“…Since expression of PD-L1 is associated with poor prognosis, a clinical trial with immune checkpoint immunotherapy seems warranted. Moreover, since the neoplastic cells and osteoclastlike giant cells are surrounded by CD163 + TAM2 that promote survival and proliferation of neoplastic cells (30), UC-OGC may be investigated as a model for testing therapies that block or "reeducate" that macrophage population (76,77). Whole exome sequencing might further provide potential treatment strategies for UC-OGC.…”

Section: Concluding Remarks and Future Perspectivesmentioning

confidence: 99%

Undifferentiated Pancreatic Carcinoma With Osteoclast-Like Giant Cells: What Do We Know So Far?

et al. 2021

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Undifferentiated carcinoma of the pancreas is an aggressive but rare tumor for which several other terms have been used to describe its histological appearance. In addition, as osteoclast-like giant cells may accompany undifferentiated carcinoma of the pancreas, the WHO Classification distinguishes undifferentiated carcinoma with osteoclast-like giant cells (UC-OGC) from plain undifferentiated carcinoma since there are a few histopathological and clinical differences. UC-OGC was initially thought to be associated with worse prognosis compared to invasive ductal pancreatic adenocarcinoma, since it is often unresectable at diagnosis and tends to recur rapidly even if completely resected. When true UC-OGGs are carefully dissected out from other anaplastic carcinomas, it becomes, however, clear that UC-OGCs do have more indolent behavior, especially the pure UC-OGCs. This mini-review summarizes the current knowledge on UC-OGC.

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Section: Concluding Remarks and Future Perspectivesmentioning

confidence: 99%

Undifferentiated Pancreatic Carcinoma With Osteoclast-Like Giant Cells: What Do We Know So Far?

et al. 2021

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“…TLR4 is one of the most important members of the TLR family and mainly expressed on the surface of mononuclear macrophages . Lipopolysaccharide (LPS) composing the outer cell wall of Gram-negative bacteria is a typical PAMP recognized by TLR4.…”

Section: Introductionmentioning

confidence: 99%

“…1 TLR4 is one of the most important members of the TLR family and mainly expressed on the surface of mononuclear macrophages. 3 Lipopolysaccharide (LPS) composing the outer cell wall of Gram-negative bacteria is a typical PAMP recognized by TLR4. LPS enters the hydrophobic pocket of co-receptor myeloid differentiation factor 2 (MD2) and induces the dimerization of TLR4-MD2, which ultimately promotes the release of NO and cytokines (e.g., TNF-α, IL-6, and IL-1β) through the NF-κB and MAPK signaling pathways.…”

Section: ■ Introductionmentioning

confidence: 99%

Identification and Molecular Mechanism of Novel Immunomodulatory Peptides from Gelatin Hydrolysates: Molecular Docking, Dynamic Simulation, and Cell Experiments

Wang

Shuian

et al. 2023

J. Agric. Food Chem.

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The purpose of this study was to identify donkey-hide gelatin-derived immunomodulatory peptides targeting Toll-like receptor 4-myeloid differentiation 2 (TLR4-MD2) and elucidate their binding modes using physicochemical property prediction, molecular docking, molecular dynamics simulations, and in vitro cell experiments. After hydrolyzing gelatin, 519 peptides were identified by liquid chromatography–tandem mass spectrometry. Peptides VQLSGEEK and GFSGLDGAKG bound to TLR4-MD2 with high binding affinity. In TLR4-MD2, Arg90, Ser118, Phe126, Tyr131, and Arg264 were key residues involved in the binding of these peptides. The RMSD and R g values demonstrated that VQLSGEEK-TLR4-MD2 and GFSGLDGAKG-TLR4-MD2 complexes had stable and compact conformations. VQLSGEEK and GFSGLDGAKG were found to increase the cell viability and phagocytic activity of RAW264.7 macrophages; significantly promote the production of cytokines TNF-α, IL-1β, and IL-6 in cells; and inhibit the overproduction of nitric oxide (NO) and cytokines in lipopolysaccharide (LPS)-induced RAW264.7 cells. Our results provided preliminary evidence that VQLSGEEK and GFSGLDGAKG could function as two-way immunomodulatory peptides with immunostimulatory and anti-inflammatory activities.

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“…Indeed, all five hub genes are important markers of macrophages. Among them, TLR4 is a classical marker of M1 macrophage polarization ( 23 ). CSF1R is an important pathway for the polarization of M2 macrophages ( 24 ).…”

Section: Discussionmentioning

confidence: 99%

Identification of Inflammation-Related Biomarkers in Diabetes of the Exocrine Pancreas With the Use of Weighted Gene Co-Expression Network Analysis

Sun

Zhang

et al. 2022

Front. Endocrinol.

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Diabetes of the exocrine pancreas (DEP), also commonly described as pancreatogenic diabetes mellitus, is a type of diabetes secondary to abnormalities in pancreatic or exocrine secretion of the pancreas. However, its pathogenesis is not yet known. The aim of this article was to explore the biomarkers of DEP and their potential molecular mechanisms. Based on GSE76896 dataset, which was acquired from Gene Expression Omnibus (GEO), we identified 373 genes by weighted gene co-expression network analysis (WGCNA) and differential expression analysis. In addition, protein–protein interaction (PPI) network analysis and cytoHubba were used to screen potential hub genes. Five hub genes were determined, comprising Toll-like receptor 4 (TLR4), ITGAM, ITGB2, PTPRC, and CSF1R. Gene Ontology (GO) analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways suggested macrophage activation and Toll-like receptor signaling pathway as important pathophysiological features of DEP. CIBERSORT suggested that TLR4 may regulate the immune pathway via macrophages. Next, we validated the expression and receiver operating characteristic curve (ROC) of the hub genes using the GSE164416 dataset. In addition, we used miRNet to predict the target miRNAs of hub genes and intersected them with common miRNAs in diabetes from the Human MicroRNA Disease Database (HMDD), which was used to propose a possible mechanistic model for DEP. The miRNA–mRNA network showed that has-miR-155-5p/has-miR-27a-3p/has-miR-21-5p-TLR4 might lead to TLR4 signaling pathway activation in DEP. In conclusion, we identified five hub genes, namely, TLR4, ITGAM, ITGB2, PTPRC, and CSF1R, as biomarkers to aid in the diagnosis of DEP and conducted an in-depth study of the pathogenesis of DEP at the genetic level.

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A novel chrysin thiazole derivative polarizes macrophages to an M1 phenotype via targeting TLR4

Cited by 10 publications

References 52 publications

Undifferentiated Pancreatic Carcinoma With Osteoclast-Like Giant Cells: What Do We Know So Far?

Undifferentiated Pancreatic Carcinoma With Osteoclast-Like Giant Cells: What Do We Know So Far?

Identification and Molecular Mechanism of Novel Immunomodulatory Peptides from Gelatin Hydrolysates: Molecular Docking, Dynamic Simulation, and Cell Experiments

Identification of Inflammation-Related Biomarkers in Diabetes of the Exocrine Pancreas With the Use of Weighted Gene Co-Expression Network Analysis

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