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Development of Fluorescent Estrogen Receptor Ligands with pH Sensor Functionality.
Tomoya Hirano1, Daisuke Yasuda1, Takeshi Yamada1
1Faculty of Pharmacy, Osaka Medical and Pharmaceutical University, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.
Chemical & Pharmaceutical Bulletin
|April 29, 2025
Summary
New fluorescent estrogen receptor ligands were developed for studying estrogen signaling and breast cancer. These novel compounds also act as pH sensors, aiding in the detection of specific pH ranges.
Area of Science:
- Medicinal Chemistry
- Molecular Biology
- Biochemistry
Background:
- Estrogen receptors (ERs) and their ligands are crucial in human physiology.
- Dysregulated ER signaling is linked to diseases like breast cancer.
- Estrogens interact with multiple receptors, including G-protein-coupled receptor 30 (GPER).
Purpose of the Study:
- To develop novel fluorescent estrogen receptor ligands for functional studies.
- To create tools for drug candidate development targeting ER signaling.
- To design ligands that can also function as pH sensors.
Main Methods:
- Synthesis of fluorescent estrogen receptor ligands based on 3-aryl-7-hydroxycoumarin.
- Characterization of ligand binding to estrogen receptors.
- Evaluation of ligand fluorescence properties and pH sensitivity.
Main Results:
- Successfully synthesized novel fluorescent estrogen receptor ligands.
- Demonstrated that these ligands bind to estrogen receptors.
- Showcased the ligands' ability to act as pH-dependent fluorescent sensors (OFF-ON-OFF type).
Conclusions:
- Developed innovative fluorescent ligands for estrogen receptor research.
- These ligands offer a dual function as probes for ER signaling and pH detection.
- Potential applications in functional studies, drug discovery, and diagnostics.
