Development of Fluorescent Estrogen Receptor Ligands with pH Sensor Functionality.

IF 1.5 4区医学 Q4 CHEMISTRY, MEDICINAL

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI:10.1248/cpb.c24-00685

Tomoya Hirano, Daisuke Yasuda, Takeshi Yamada, Hiroyuki Kagechika

引用次数: 0

Abstract

Estrogen receptors (ERs) and their ligands regulate a variety of physiological processes in humans, and altered ER signaling is associated with serious disorders, including breast cancer. Estrogens also bind to other receptors such as G-protein-coupled receptor 30 (GPER), and so fluorescent estrogen ligands would be useful for various functional studies and for development of drug candidates. Here we describe fluorescent estrogen receptor ligands based on 3-aryl-7-hydroxycoumarin. Notably, these ligands also function as pH-dependent OFF-ON-OFF type fluorescent sensors, enabling the detection of specific ranges of pH.

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具有pH传感器功能的荧光雌激素受体配体的研制。

雌激素受体（ER）及其配体调节人体多种生理过程，雌激素受体信号的改变与包括乳腺癌在内的严重疾病有关。雌激素还与其他受体结合，如g蛋白偶联受体30 (GPER)，因此荧光雌激素配体将有助于各种功能研究和候选药物的开发。本文描述了基于3-芳基-7-羟基香豆素的荧光雌激素受体配体。值得注意的是，这些配体还作为pH依赖的OFF-ON-OFF型荧光传感器，能够检测特定的pH范围。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Chemical & pharmaceutical bulletin 医学-化学综合

CiteScore

3.20

自引率

5.90%

发文量

132

审稿时长

1.7 months

期刊介绍： The CPB covers various chemical topics in the pharmaceutical and health sciences fields dealing with biologically active compounds, natural products, and medicines, while BPB deals with a wide range of biological topics in the pharmaceutical and health sciences fields including scientific research from basic to clinical studies. For details of their respective scopes, please refer to the submission topic categories below. Topics: Organic chemistry In silico science Inorganic chemistry Pharmacognosy Health statistics Forensic science Biochemistry Pharmacology Pharmaceutical care and science Medicinal chemistry Analytical chemistry Physical pharmacy Natural product chemistry Toxicology Environmental science Molecular and cellular biology Biopharmacy and pharmacokinetics Pharmaceutical education Chemical biology Physical chemistry Pharmaceutical engineering Epidemiology Hygiene Regulatory science Immunology and microbiology Clinical pharmacy Miscellaneous.