Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Background: 2-Methoxystypandrone (2-MS), isolated from the roots of Polygonum cuspidatum, is a potent dual inhibitor of the STAT3 and NF-κB pathways.
Objective: To investigate the molecular targets and mechanisms of 2-MS.
Method: A biotin-conjugated 2-MS analog, named 2-MS-Biotin, was designed and synthesized. The effects of 2-MS-Biotin on the STAT3 and NF-κB pathways were examined by Western blotting. The cytotoxicity of 2- MS-Biotin was evaluated using real-time cell analysis system. Proteins directly bound to 2-MS-Biotin were pulled down through streptavidin agarose beads and were detected using Western blotting.
Results: 2-MS-Biotin retained the inhibition activities of the parent compound 2-MS on the STAT3 and NF-κB pathways as well as on cancer cell growth. Also, JAK2 and IKK proteins can be effectively pulled down by 2- MS-Biotin.
Conclusion: Using 2-MS-Biotin as a tool, both JAK2 and IKK were identified as the targets of 2-MS.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.2174/1871520617666171106123226 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Anthocyanin Extracts Improve Hepatic Structure and Function in High-Fat Diet-/Streptozotocin-Induced T2DM Mice.
J Agric Food Chem
September 2022
College of Food Science, Shenyang Agricultural University, Shenyang, Liaoning 110866, P. R. China.
Anthocyanins can prevent and ameliorate type 2 diabetes mellitus (T2DM), but its mechanism of action has not been fully established. IKK/NF-κB and JAK/Stat pathways have multiple effects, triggering T2DM. Liver abnormalities in individuals with T2DM are detrimental to glycemic control.
View Article and Find Full Text PDFHeterogeneity of Platelet Derived Growth Factor Pathway Gene Expression Profile Defines Three Distinct Subgroups of Renal Cell Carcinomas.
Cancer Genomics Proteomics
June 2022
Department of Microscopic Morphology/Histology, Victor Babes University of Medicine and Pharmacy, Timisoara, Romania.
Background/aim: We previously described four different vascular patterns (reticular, diffuse, fasciculate, and trabecular) in renal cell carcinoma (RCC) suggesting an early and heterogeneous acquisition of perivascular cells most probably due to a particular PDGF pathway gene expression profile. The aim of the study was to study PDGF pathway gene expression profiles, separately for each vascular pattern.
Materials And Methods: TaqMan assay for the PDGF pathway was performed on twelve cases of ccRCC previously evaluated by histopathology, immunohistochemistry, and RNAscope.
Anti-inflammatory Effects of Empagliflozin and Gemigliptin on LPS-Stimulated Macrophage via the IKK/NF-B, MKK7/JNK, and JAK2/STAT1 Signalling Pathways.
J Immunol Res
December 2021
Department of Endocrinology and Metabolism, Ajou University School of Medicine, Suwon, Republic of Korea.
Article Synopsis
- Empagliflozin (SGLT2 inhibitor) and gemigliptin (DPP-4 inhibitor) have been found to reduce inflammation in macrophages, which could help with conditions like diabetes and obesity, alongside their glucose-lowering effects.
- The study involved treating macrophages with these drugs after stimulating inflammation with lipopolysaccharide (LPS) and measuring the resulting changes in inflammatory markers.
- Results showed that both empagliflozin and gemigliptin, alone and in combination, significantly decreased pro-inflammatory cytokines and chemokines, while also inhibiting key inflammatory signaling pathways like NF-κB and MAPK.
Down-Regulation of LOC645166 in T Cells of Ankylosing Spondylitis Patients Promotes the NF-κB Signaling Decreasingly Blocking Recruitment of the IKK Complex to K63-Linked Polyubiquitin Chains.
Front Immunol
July 2021
Department of Biomedical Sciences, National Chung Cheng University, Chiayi, Taiwan.
Ankylosing spondylitis (AS) is a chronic inflammatory disease that mainly affects the spine. AS is highly associated with the expression of HLA-B27. Up to 95% AS patients are HLA-B27-positive.
View Article and Find Full Text PDFThe Effects of Sidt2 on the Inflammatory Pathway in Mouse Mesangial Cells.
Mediators Inflamm
July 2021
Department of Endocrinology and Genetic Metabolism, Yijishan Hospital of Wannan Medical College, Wuhu 241002, China.
In patients with chronic kidney disease, the abnormal activation of inflammatory pathways is usually an important factor leading to renal fibrosis and further deterioration of renal function. Finding effective intervention targets of the inflammatory signaling pathway is an important way to treat chronic kidney disease. As a newly discovered lysosomal membrane protein, the correlation between SID1 transmembrane family member 2 (Sidt2) and the inflammatory signaling pathway has not been reported.
View Article and Find Full Text PDF