論文 - 詳細
| RRC ID | 44339 |
|---|---|
| 著者 | Niino S, Nakamura Y, Hirabayashi Y, Nagano-Ito M, Ichikawa S. |
| タイトル | A small molecule inhibitor of Bcl-2, HA14-1, also inhibits ceramide glucosyltransferase. |
| ジャーナル | Biochem Biophys Res Commun |
| Abstract |
HA14-1 is a Bcl-2 inhibitor that is widely used for studies of apoptosis. In the course of searching for a ceramide glucosyltransferase inhibitor that catalyzes the first glycosylation step of glycosphingolipid synthesis, we unexpectedly found that HA-14-1 also has the ability to inhibit ceramide glucosyltransferase. The IC50 value of HA14-1 against ceramide glucosyltransferase is 4.5μM, which is lower than that reported for Bcl-2 in vitro. Kinetic analyses revealed that HA14-1 is a competitive and mixed-type inhibitor with respect to C6-NBD-ceramide and UDP-glucose, respectively. |
| 巻・号 | 433(2) |
| ページ | 170-4 |
| 公開日 | 2013-4-5 |
| DOI | 10.1016/j.bbrc.2013.02.052 |
| PII | S0006-291X(13)00312-4 |
| PMID | 23485465 |
| MeSH | 4-Chloro-7-nitrobenzofurazan / analogs & derivatives 4-Chloro-7-nitrobenzofurazan / pharmacology Animals Apoptosis / drug effects Benzopyrans / pharmacology* Cell Line Ceramides / metabolism Ceramides / pharmacology Drug Evaluation, Preclinical / methods Enzyme Inhibitors / pharmacology Glucosyltransferases / antagonists & inhibitors* Glucosyltransferases / metabolism Humans Inhibitory Concentration 50 Kinetics Melanoma, Experimental / drug therapy Melanoma, Experimental / metabolism Mice Nitriles / pharmacology* Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors |
| IF | 2.985 |
| 引用数 | 4 |
| WOS 分野 | BIOPHYSICS BIOCHEMISTRY & MOLECULAR BIOLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 3 |
| 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 | B16 melanoma |