Linkage Effects on Binding Affinity and Activation of GPR30 and Estrogen Receptors ER/
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- 作者：Chinnasamy Ramesh ; Bj Bryant ; Tapan Nayak ; Chetana M. Revankar ; Tamara Anderson ; Kathryn E. Carlson ; John A. Katzenellenbogen ; Larry A. Sklar ; Jeffrey P. Norenberg ; Eric R. Prossnitz ; Jeffrey B. Arterb
- 刊名：Journal of the American Chemical Society
- 出版年：2006
- 出版时间：November 15, 2006
- 年：2006
- 卷：128
- 期：45
- 页码：14476 - 14477
- 全文大小：63K
- 年卷期：v.128,no.45(November 15, 2006)
- ISSN：1520-5126
文摘
We describe a new structural class of neutral tridentate pyridin-2-yl hydrazine chelates for labeling with tricarbonyl Re/99mTc(I) under aqueous conditions and investigate the receptor binding of synthetic estradiol derivatives with the novel G-protein-coupled receptor GPR30 and estrogen receptors ER
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beta2.gif" BORDER=0 ALIGN="middle">. The steroid linkage affected the affinity and selectivity of estrogen binding with these receptors. Fluorescence assays based on calcium signaling demonstrate that membrane-permeable chelates 2 and 3 interact with the receptors in whole cells. These results suggest that in vitro assays will facilitate the development of targeted imaging agents for intracellular receptors and the feasibility of targeting GPR30 and ER/beta2.gif" BORDER=0 ALIGN="middle"> for diagnostic tumor imaging.
/beta2.gif" BORDER=0 ALIGN="middle">. The steroid linkage affected the affinity and selectivity of estrogen binding with these receptors. Fluorescence assays based on calcium signaling demonstrate that membrane-permeable chelates 2 and 3 interact with the receptors in whole cells. These results suggest that in vitro assays will facilitate the development of targeted imaging agents for intracellular receptors and the feasibility of targeting GPR30 and ER/beta2.gif" BORDER=0 ALIGN="middle"> for diagnostic tumor imaging.