Development of an Environmentally Responsive Fluorescent Ligand for Vitamin D Receptor

被引：0

作者：

Iwaki, Miho ^{[1
]}

Sakamoto, Ryota ^{[1
]}

Tsutsumi, Rino ^{[1
]}

Sawada, Takahiro ^{[2
,3
]}

Hirokawa, Takatsugu ^{[4
,5
]}

Kato, Shigeaki ^{[2
,3
,6
]}

Nagasawa, Kazuo ^{[1
]}

机构：

[1] Tokyo Univ Agr & Technol, Fac Engn, Dept Biotechnol & Life Sci, 2-24-16,Naka Cho, Koganei, Tokyo 1848588, Japan

[2] Iryo Sosei Univ, Grad Sch Life Sci & Engn, Iwaki, Fukushima 9708551, Japan

[3] Tokiwa Fdn, Res Inst Innovat Med, Iwaki, Fukushima, Japan

[4] Univ Tsukuba, Transborder Med Res Ctr, 1-1-1 Tennodai, Tsukuba 3058575, Japan

[5] Univ Tsukuba, Fac Med, Div Biomed Sci, 1-1-1 Tennodai, Tsukuba 3058575, Japan

[6] Fukushima Med Univ, Sch Med, Fukushima 9601295, Japan

来源：

CHEMBIOCHEM | 2025年 / 26卷 / 08期

关键词：

Fluorescent probes; Bioorganic chemistry; Vitamin D-3; Vitamin D receptor; Environmentally responsive fluorescent probe; 1-ALPHA; 25-DIHYDROXYVITAMIN D-3; ACCURATE DOCKING; ANALOGS; BINDING; ROUTE; GLIDE;

D O I：

10.1002/cbic.202401038

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Vitamin D receptor (VDR) plays a critical role in regulating multiple biological processes, including bone metabolism and cell differentiation, by mediating transcriptional activation in response to ligand binding. We have constructed an environmentally fluorescent probe 2 for VDR to facilitate real-time observation of its ligand-dependent conformational changes in living cells. This probe 2 was synthesized by introducing a dansyl fluorophore via an ethynyl group at the C11 position of 1 alpha,25(OH)(2)D-3. Probe 2 exhibited strong environmentally responsive fluorescence, showing increased intensity and a blue shift of the peak wavelength upon binding to VDR due to the increased hydrophobicity of the environment.

引用

页数：5

共 32 条

[1]

Andrey K. S, 2017, Acc. Chem. Res., V50, P366

[2] DEVELOPMENT OF A BIOLOGICALLY-ACTIVE FLUORESCENT-LABELED CALCITRIOL AND ITS USE TO STUDY HORMONE-BINDING TO THE VITAMIN-D-RECEPTOR [J].