Linkage effects on binding affinity and activation of GPR30 and estrogen receptors ERα/β with tridentate pyridin-2-yl hydrazine tricarbonyl-Re/99mTc(I) chelates

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. Arterburn

Research output: Contribution to journalArticlepeer-review

Abstract

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 ERα/β. 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 ERα/β for diagnostic tumor imaging.

Original languageEnglish (US)
Pages (from-to)14476-14477
Number of pages2
JournalJournal of the American Chemical Society
Volume128
Issue number45
DOIs
StatePublished - Nov 15 2006

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)
  • Biochemistry
  • Colloid and Surface Chemistry

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