S14-95, a novel inhibitor of the JAK/STAT pathway from a Penicillium species.
(2003) In Journal of Antibiotics 56(4). p.337-343- Abstract
- In a search for new inhibitors of the IFN-γ mediated signal transduction in HeLa S3 cells using secreted alkaline phosphatase (SEAP) as reporter gene, a novel compound, designated as S14-95 was isolated from fermentations of the imperfect fungus Penicillium sp. 14-95. The compound inhibits the IFN-γ mediated expression of the reporter gene with IC50 values of 2.5~5μg/ml (5.4~10.8μM). Furthermore the compound inhibited the expression of the proinflammatory enzymes COX-2 and NOS II at 5μg/ml (10.8μM) in LPS/IFN-γ stimulated J774 mouse macrophages. Studies on the mode of action of the compound revealed that the inhibition of the IFN-γ dependent signaling pathway is caused by an inhibition of the phosphorylation of the STAT1α transcription... (More)
- In a search for new inhibitors of the IFN-γ mediated signal transduction in HeLa S3 cells using secreted alkaline phosphatase (SEAP) as reporter gene, a novel compound, designated as S14-95 was isolated from fermentations of the imperfect fungus Penicillium sp. 14-95. The compound inhibits the IFN-γ mediated expression of the reporter gene with IC50 values of 2.5~5μg/ml (5.4~10.8μM). Furthermore the compound inhibited the expression of the proinflammatory enzymes COX-2 and NOS II at 5μg/ml (10.8μM) in LPS/IFN-γ stimulated J774 mouse macrophages. Studies on the mode of action of the compound revealed that the inhibition of the IFN-γ dependent signaling pathway is caused by an inhibition of the phosphorylation of the STAT1α transcription factor. In addition, S14-95 inhibited the activation of the p38 MAP kinase, which is involved in the inducible expression of many proinflammatory genes. (Less)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/127921
- author
- Erkel, G ; Rether, J ; Anke, T and Sterner, Olov LU
- organization
- publishing date
- 2003
- type
- Contribution to journal
- publication status
- published
- subject
- in
- Journal of Antibiotics
- volume
- 56
- issue
- 4
- pages
- 337 - 343
- publisher
- Japan Antibiotics Research Association
- external identifiers
-
- wos:000182565800001
- pmid:12817806
- scopus:0037959568
- ISSN
- 0021-8820
- language
- English
- LU publication?
- yes
- additional info
- The information about affiliations in this record was updated in December 2015. The record was previously connected to the following departments: Organic chemistry (S/LTH) (011001240)
- id
- 8ea5ee20-9a8e-427a-83a4-eb91045fc6ca (old id 127921)
- alternative location
- http://www.antibiotics.or.jp/journal/contents/vol-56/abstract/56-4/ja560401.htm
- http://www.antibiotics.or.jp/journal/contents/vol-56/56contents_1.htm#febraury
- date added to LUP
- 2016-04-01 15:46:32
- date last changed
- 2022-01-28 07:00:26
@article{8ea5ee20-9a8e-427a-83a4-eb91045fc6ca,
abstract = {{In a search for new inhibitors of the IFN-γ mediated signal transduction in HeLa S3 cells using secreted alkaline phosphatase (SEAP) as reporter gene, a novel compound, designated as S14-95 was isolated from fermentations of the imperfect fungus Penicillium sp. 14-95. The compound inhibits the IFN-γ mediated expression of the reporter gene with IC50 values of 2.5~5μg/ml (5.4~10.8μM). Furthermore the compound inhibited the expression of the proinflammatory enzymes COX-2 and NOS II at 5μg/ml (10.8μM) in LPS/IFN-γ stimulated J774 mouse macrophages. Studies on the mode of action of the compound revealed that the inhibition of the IFN-γ dependent signaling pathway is caused by an inhibition of the phosphorylation of the STAT1α transcription factor. In addition, S14-95 inhibited the activation of the p38 MAP kinase, which is involved in the inducible expression of many proinflammatory genes.}},
author = {{Erkel, G and Rether, J and Anke, T and Sterner, Olov}},
issn = {{0021-8820}},
language = {{eng}},
number = {{4}},
pages = {{337--343}},
publisher = {{Japan Antibiotics Research Association}},
series = {{Journal of Antibiotics}},
title = {{S14-95, a novel inhibitor of the JAK/STAT pathway from a Penicillium species.}},
url = {{http://www.antibiotics.or.jp/journal/contents/vol-56/abstract/56-4/ja560401.htm}},
volume = {{56}},
year = {{2003}},
}