Synthesis and characterization of 5,7-dihydroxyflavanone derivatives as novel protein tyrosine phosphatase 1B inhibitors
文献类型：期刊论文
| 作者 | Sun, Liang-Peng2; Ma, Wei-Ping1; Gao, Li-Xin1; Yang, Ling-Ling1; Quan, Ying-Chun2; Li, Jia1 ; Piao, Hu-Ri2
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| 刊名 | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
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| 出版日期 | 2013-12 |
| 卷号 | 28期号:6页码:1199-1204 |
| 关键词 | Protein tyrosine phosphatase 1B inhibitors 5,7-dihydroxyflavanone structure-activity relationship diabetes |
| ISSN号 | 1475-6366 |
| DOI | 10.3109/14756366.2012.723206 |
| 文献子类 | Article |
| 英文摘要 | A series of 5,7-dihydroxyflavanone derivatives were synthesized and identified as reversible and competitive protein tyrosine phosphatase (PTP) 1B inhibitors with IC50 values in the micromolar range. Compound 4k had the most potent in vitro inhibition activity against PTP1B (IC50 = 2.37 +/- 0.37 mu M) and the greatest selectivity (3.7-fold) for PTP1B relative to T-cell protein tyrosine phosphatase. Cell-based studies revealed that 4k was membrane-permeable and enhanced insulin receptor tyrosine phosphorylation in CHO/hIR cells. |
| WOS关键词 | STRUCTURAL REQUIREMENTS ; INSULIN SENSITIVITY ; ISOPRENYLATED FLAVONOIDS ; ERYTHRINA-ABYSSINICA ; STEM BARK ; OBESITY ; PTP1B ; MICE ; RESISTANCE ; CANCER |
| 资助项目 | National Natural Science Foundation of China[20962021] ; National Natural Science Foundation of China[81125023] ; National Program on Key Basic Research Project of China (973 Program)[2012CB524906] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000326745800009 |
| 出版者 | INFORMA HEALTHCARE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277363]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物安全性评价中心 |
| 通讯作者 | Piao, Hu-Ri |
| 作者单位 | 1.Chinese Acad Sci, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai Inst Mat Med,Shanghai Inst Biol Sci, Shanghai, Peoples R China 2.Yanbian Univ, Coll Pharm, Key Lab Nat Resources Changbai Mt & Funct Mol, Yanji 133000, Jilin Province, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Sun, Liang-Peng,Ma, Wei-Ping,Gao, Li-Xin,et al. Synthesis and characterization of 5,7-dihydroxyflavanone derivatives as novel protein tyrosine phosphatase 1B inhibitors[J]. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,2013,28(6):1199-1204. |
| APA | Sun, Liang-Peng.,Ma, Wei-Ping.,Gao, Li-Xin.,Yang, Ling-Ling.,Quan, Ying-Chun.,...&Piao, Hu-Ri.(2013).Synthesis and characterization of 5,7-dihydroxyflavanone derivatives as novel protein tyrosine phosphatase 1B inhibitors.JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY,28(6),1199-1204. |
| MLA | Sun, Liang-Peng,et al."Synthesis and characterization of 5,7-dihydroxyflavanone derivatives as novel protein tyrosine phosphatase 1B inhibitors".JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY 28.6(2013):1199-1204. |
入库方式： OAI收割
来源：上海药物研究所
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