Competitive binding assays for measuring the binding affinity of thyroid-disrupting chemicals for integrin alpha(v)beta(3)
文献类型：期刊论文
| 作者 | Li, Jian; Liu, Hedan; Zuo, Rui; Yang, Jie; Li, Na
|
| 刊名 | CHEMOSPHERE
 |
| 出版日期 | 2020-06 |
| 卷号 | 249页码:1-8 |
| 关键词 | Thyroid-disrupting chemicals Integrin alpha(v)beta(3) Competitive binding assay T4-BSA-F Tc-99m-3PRGD(2) Phthalate esters |
| ISSN号 | 0045-6535 |
| 英文摘要 | Some thyroid-disrupting chemicals (TDCs) affect thyroid function by activating the pathways mediated by a typical thyroid hormone (TH) membrane receptor, integrin alpha(v)beta(3). The present study introduces improved competitive binding assays for the rapid and sensitive evaluation of the binding affinities of TDCs for integrin alpha(v)beta(3). Based on different probes, two assays were modified: a fluorescence competitive binding assay and a radioligand competitive binding assay. The chemicals tested included the known TH, 3,3',5,5'-tetraiodo-L-thyronine (T4); a deaminated analog of T4, tetraiodothyroacetic acid (tetrac); and phthalate esters (PAEs). The relative binding potency of T4 was studied, and the concentration required to displace 50% of the ligands from their receptors (RIC50) of T4 was 4.9 x 10(5) and 9.7 x 10(4) nM for the fluorescence and radioligand competitive binding assays, respectively, suggesting that the radioligand competitive binding assay might be more sensitive for the evaluation of the binding affinity for integrin alpha(v)beta(3). The three PAEs, including diethyl hexyl phthalate (DEHP), benzyl butyl phthalate (BBP) and dibutyl phthalate (DnBP), demonstrated binding affinities for integrin alpha(v)beta(3) in the following order of potency: DnBP > DEHP > BBP tested by the radioligand competitive binding assay. A docking simulation of each of the three PAEs with integrin alpha(v)beta(3) confirmed the calculated binding energies, which had a strong positive relationship with the log RIC20 values of the 3 PAEs (R = 0.99, p < 0.001). The present study shows that the established radioligand competitive binding assay could be used as a valuable tool for quantifying the affinity of TDCs for integrin alpha(v)beta(3). (C) 2020 Published by Elsevier Ltd. |
| 源URL | [http://ir.rcees.ac.cn/handle/311016/45256]  |
| 专题 | 生态环境研究中心_中国科学院饮用水科学与技术重点实验室 |
| 推荐引用方式 GB/T 7714 | Li, Jian,Liu, Hedan,Zuo, Rui,et al. Competitive binding assays for measuring the binding affinity of thyroid-disrupting chemicals for integrin alpha(v)beta(3)[J]. CHEMOSPHERE,2020,249:1-8. |
| APA | Li, Jian,Liu, Hedan,Zuo, Rui,Yang, Jie,&Li, Na.(2020).Competitive binding assays for measuring the binding affinity of thyroid-disrupting chemicals for integrin alpha(v)beta(3).CHEMOSPHERE,249,1-8. |
| MLA | Li, Jian,et al."Competitive binding assays for measuring the binding affinity of thyroid-disrupting chemicals for integrin alpha(v)beta(3)".CHEMOSPHERE 249(2020):1-8. |
入库方式： OAI收割
来源：生态环境研究中心
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