HL005-A new selective PPAR gamma antagonist specifically inhibits the proliferation of MCF-7
文献类型：期刊论文
| 作者 | Lu, Weiqiang2; Che, Peng2; Zhang, Yanyan2; Li, Honglin2; Zou, Shien1; Zhu, Jin2; Deng, Jing2; Shen, Xu2,3 ; Jiang, Hualiang2,3; Li, Jian2
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| 刊名 | JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
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| 出版日期 | 2011-04 |
| 卷号 | 124期号:3-5页码:112-120 |
| 关键词 | Peroxisome proliferator-activated receptor-gamma Selective antagonist Anticancer Apoptosis |
| ISSN号 | 0960-0760 |
| DOI | 10.1016/j.jsbmb.2011.01.019 |
| 文献子类 | Article |
| 英文摘要 | Peroxisome proliferator-activated receptor-gamma (PPAR gamma) is a nuclear transcription factor which is involved in many diseases, such as diabetes, inflammation, dyslipidemia. hypertension, and cancer. Recently, there are many reports showing that PPAR gamma agonists have preclinical and clinical anticancer activity, with relatively few reports on anticancer effects of PPAR gamma antagonists. From our compound library, a novel 3-thiazolinone-modified benzoic acid derivative HL005 is found as PPAR gamma selective ligand through SPR analysis (K-D = 0.21 mu M), yeast two-hybrid results suggest that HL005 antagonize the potent PPAR gamma agonist rosiglitazone-induced recruitment of the coactivator for PPAR gamma (IC50 = 7.97 mu M). Different from the most reported PPAR gamma antagonist, HL005 can inhibit the proliferation of MCF-7 cell line in a concentration-dependent manner and induce cell cycle arrest at G2/M phase, other than interference with cell adhesion. In order to study the binding mode of this compound, three derivatives are synthesized to get more detail about the structure-activity relationship, molecular docking and the NMR spectra indicate that similar to most PPAR gamma ligand, the carboxylic acid group is an important moiety for HL005 and contributes strong interaction with PPAR gamma. (C) 2011 Elsevier Ltd. All rights reserved. |
| WOS关键词 | ACTIVATED-RECEPTOR-GAMMA ; BREAST-CANCER CELLS ; CARCINOMA CELLS ; INDUCE APOPTOSIS ; GENE-EXPRESSION ; IN-VITRO ; LIGANDS ; TROGLITAZONE ; GROWTH ; ALPHA |
| 资助项目 | Shanghai Pujiang Program[PJ200700247] ; Shanghai Municipal Education Commission[10ZZ41] ; Shanghai Committee of Science and Technology[08JC1407800] ; National Natural Science Foundation of China[90813005] ; National Natural Science Foundation of China[10979072] ; 111 Project[B07023] ; 863 Hi-Tech Program of China[2007AA02Z147] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Endocrinology & Metabolism |
| 语种 | 英语 |
| WOS记录号 | WOS:000289660100006 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278567]  |
| 专题 | 药物发现与设计中心 |
| 通讯作者 | Li, Jian |
| 作者单位 | 1.Fudan Univ, Obstet & Gynecol Hosp, Shanghai 200011, Peoples R China; 2.E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lu, Weiqiang,Che, Peng,Zhang, Yanyan,et al. HL005-A new selective PPAR gamma antagonist specifically inhibits the proliferation of MCF-7[J]. JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,2011,124(3-5):112-120. |
| APA | Lu, Weiqiang.,Che, Peng.,Zhang, Yanyan.,Li, Honglin.,Zou, Shien.,...&Huang, Jin.(2011).HL005-A new selective PPAR gamma antagonist specifically inhibits the proliferation of MCF-7.JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY,124(3-5),112-120. |
| MLA | Lu, Weiqiang,et al."HL005-A new selective PPAR gamma antagonist specifically inhibits the proliferation of MCF-7".JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY 124.3-5(2011):112-120. |
入库方式： OAI收割
来源：上海药物研究所
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