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Vialinin A and thelephantin G, potent inhibitors of tumor necrosis factor-α production, inhibit sentrin/SUMO-specific protease 1 enzymatic activity
- Source :
- Bioorganic & Medicinal Chemistry Letters. 26:4237-4240
- Publication Year :
- 2016
- Publisher :
- Elsevier BV, 2016.
-
Abstract
- Several p-terphenyl compounds have been isolated from the edible Chinese mushroom Thelephora vialis. Vialinin A, a p-terphenyl compound, strongly inhibits tumor necrosis factor-α production and release. Vialinin A inhibits the enzymatic activity of ubiquitin-specific peptidase 5, one of the target molecules in RBL-2H3 cells. Here we examined the inhibitory effect of p-terphenyl compounds, including vialinin A, against sentrin/SUMO-specific protease 1 (SENP1) enzymatic activity. The half maximal inhibitory concentration values of vialinin A and thelephantin G against full-length SENP1 were 1.64±0.23μM and 2.48±0.02μM, respectively. These findings suggest that p-terphenyl compounds are potent SENP1 inhibitors.
- Subjects :
- 0301 basic medicine
SENP1
medicine.medical_treatment
SUMO-1 Protein
Clinical Biochemistry
Pharmaceutical Science
Plasma protein binding
Biochemistry
Cell Line
law.invention
03 medical and health sciences
law
Terphenyl Compounds
Drug Discovery
medicine
Animals
Humans
Molecular Biology
chemistry.chemical_classification
Protease
030102 biochemistry & molecular biology
biology
Tumor Necrosis Factor-alpha
Chemistry
Organic Chemistry
Recombinant Proteins
Enzyme assay
Rats
Kinetics
030104 developmental biology
Enzyme
Cell culture
biology.protein
Recombinant DNA
Molecular Medicine
Tumor necrosis factor alpha
Agaricales
Protein Binding
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 26
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....0e80c349436e46657e06847958116671