کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9920901 | 1559194 | 2005 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
EK-6136 (3-methyl-4-(O-methyl-oximino)-1-phenylpyrazolin-5-one): A novel Cdc25B inhibitor with antiproliferative activity
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موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: EK-6136 (3-methyl-4-(O-methyl-oximino)-1-phenylpyrazolin-5-one): A novel Cdc25B inhibitor with antiproliferative activity EK-6136 (3-methyl-4-(O-methyl-oximino)-1-phenylpyrazolin-5-one): A novel Cdc25B inhibitor with antiproliferative activity](/preview/png/9920901.png)
چکیده انگلیسی
Cdc25B is a dual specific phosphatase, which plays a pivotal role in the activation of cell-cycle-dependent kinase 1 (Cdk1). A novel Cdc25B inhibitor, EK-6136, was identified by high throughput screening (HTS) using compounds from Korea Chemical Bank and examined for its biological effects. EK-6136 inhibited Cdc25B with an IC50 of 6.4 ± 1.5 μM. EK-6136 showed selectivity against several phosphatases including PTP-1B, CD45, Cdc25A, PP1, VHR and Yop. In the inhibition kinetic study, EK-6136 displayed a mixed inhibition pattern with a Ki value of 7.8 ± 1.2 μM. Consistent with in vitro results, EK-6136 inhibited the proliferation of MCF-7 (human breast carcinoma), HT-29 (human colorectal adenocarcinoma) and A549 (lung carcinoma) cells with increased Cdk-1 phosphorylation. Herein, we propose that EK-6136 is an active HTS hit as a Cdc25B inhibitor with antiproliferative activity, and can be used for the design of more potent and selective antiproliferative agents.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 528, Issues 1â3, 28 December 2005, Pages 37-42
Journal: European Journal of Pharmacology - Volume 528, Issues 1â3, 28 December 2005, Pages 37-42
نویسندگان
Kwang-Rok Kim, Ju-Lee Kwon, Ji-Sun Kim, Zaesung No, Hyoung Rae Kim, Hyae Gyeong Cheon,