Determining PPAR gamma-ligand binding affinity using fluorescent assay with cis-parinaric acid as a probe
文献类型：期刊论文
| 作者 | Gao, ZT; Luo, HB; Chen, LL ; Shen, JH; Chen, KX; Jiang, HL; Shen, X
|
| 刊名 | SCIENCE IN CHINA SERIES B-CHEMISTRY
 |
| 出版日期 | 2005-04 |
| 卷号 | 48期号:2页码:122-131 |
| 关键词 | displacement assay IC50 equilibrium dissociation constant PPAR gamma cis-parinaric acid fluorescent probe |
| ISSN号 | 1006-9291 |
| DOI | 10.1360/03yb0217 |
| 文献子类 | Article |
| 英文摘要 | Upon the study of small-molecules binding to proteins, the traditional methods for calculating dissociation constants (K-d and K-i) have shortcomings in dealing with the single binding site models. In this paper, two equations have been derived to solve this problem. These two equations are independent of the total concentration or initial degree of saturation of receptor and the activity of the competitive molecule. Through nonlinear fitting against these two equations, K-d value of a probe can be obtained by binding assay, and K-i value of a ligand can be obtained by competitive assay. Moreover, only the total concentrations of receptor([R](t)), ligand([L](t)) and probe([P](t)) are required for the data fitting. In this work, K-i values of some typical ligands of PPAR gamma were successfully determined by use of our equations, among which the K-i value of PPAR gamma-LY171883 was reported for the first time. |
| WOS关键词 | ACTIVATED RECEPTOR-GAMMA ; FATTY-ACIDS ; ALPHA ; DISCOVERY ; AGONISTS |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000229230700005 |
| 出版者 | SCIENCE CHINA PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273891]  |
| 专题 | 药物发现与设计中心 药理学第三研究室 |
| 通讯作者 | Jiang, HL |
| 作者单位 | 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 | Gao, ZT,Luo, HB,Chen, LL,et al. Determining PPAR gamma-ligand binding affinity using fluorescent assay with cis-parinaric acid as a probe[J]. SCIENCE IN CHINA SERIES B-CHEMISTRY,2005,48(2):122-131. |
| APA | Gao, ZT.,Luo, HB.,Chen, LL.,Shen, JH.,Chen, KX.,...&Shen, X.(2005).Determining PPAR gamma-ligand binding affinity using fluorescent assay with cis-parinaric acid as a probe.SCIENCE IN CHINA SERIES B-CHEMISTRY,48(2),122-131. |
| MLA | Gao, ZT,et al."Determining PPAR gamma-ligand binding affinity using fluorescent assay with cis-parinaric acid as a probe".SCIENCE IN CHINA SERIES B-CHEMISTRY 48.2(2005):122-131. |
入库方式： OAI收割
来源：上海药物研究所
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