論文 - 詳細
| RRC ID | 43895 |
|---|---|
| 著者 | Umehara H, Asai A. |
| タイトル | Tributylhexadecylphosphonium bromide, a novel nuclear factor of activated T cells signaling inhibitor, blocks interleukin-2 induction associated with inhibition of p70 ribosomal protein S6 kinase phosphorylation. |
| ジャーナル | Biol Pharm Bull |
| Abstract |
Transcriptional factors of the nuclear factor of activated T cells (NFAT) family are involved in T cell signaling. Many NFAT signaling inhibitors, such as cyclosporin A (CsA) and tacrolimus, abrogate dephosphorylation of NFAT proteins by inhibiting calcineurin activity. In pursuit of a novel type of NFAT signaling inhibitor, we screened our chemical library using the NFAT-dependent reporter assay and identified tributylhexadecylphosphonium bromide (THPB) as a selective NFAT signaling inhibitor. THPB inhibited NFAT-dependent reporter activity, and the induction of interleukin-2 (IL-2) at both mRNA and protein levels by calcium stimulation. Moreover, THPB had an additive effect on the inhibition of IL-2 induction with CsA. Unlike CsA, THPB did not affect dephosphorylation of NFAT1, but suppressed phosphorylation of p70 ribosomal protein S6 kinase (p70S6K). These results suggest that THPB may be a novel type of NFAT signaling inhibitor that acts in association with inhibition of p70S6K phosphorylation. |
| 巻・号 | 35(5) |
| ページ | 805-9 |
| 公開日 | 2012-1-1 |
| DOI | 10.1248/bpb.35.805 |
| PII | JST.JSTAGE/bpb/35.805 |
| PMID | 22687422 |
| MeSH | Calcium / pharmacology* Cyclosporine / pharmacology* Humans Interleukin-2 / genetics Interleukin-2 / metabolism* Jurkat Cells NFATC Transcription Factors / antagonists & inhibitors* Organophosphorus Compounds / pharmacology* Phosphorylation / drug effects RNA, Messenger / metabolism Ribosomal Protein S6 Kinases, 70-kDa / antagonists & inhibitors* Signal Transduction / drug effects T-Lymphocytes / drug effects* T-Lymphocytes / metabolism |
| IF | 1.863 |
| 引用数 | 3 |
| WOS 分野 | PHARMACOLOGY & PHARMACY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
|
| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 1 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | Jurkat |