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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

Authors :
Jun-ichi Onose
Hitoshi Ashida
Mao Makiuchi
Yasukiyo Yoshioka
Daisuke Namiki
Kouichi Sugaya
Naoki Abe
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.

Details

ISSN :
0960894X
Volume :
26
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....0e80c349436e46657e06847958116671