| 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
|
| リソース情報 |
| ヒト・動物細胞 |
|
