Development of an environmentally responsive fluorescent ligand for vitamin D receptor

Kazuo Nagasawa; Miho Iwaki; Ryota Sakamoto; Rino Tsutsumi; Takahiro Sawada; Takatsugu Hirokawa; Shigeaki Kato

doi:10.1002/cbic.202401038

Development of an environmentally responsive fluorescent ligand for vitamin D receptor

Chembiochem. 2025 Jan 22:e202401038. doi: 10.1002/cbic.202401038. Online ahead of print.

Authors

Kazuo Nagasawa¹, Miho Iwaki², Ryota Sakamoto², Rino Tsutsumi², Takahiro Sawada³, Takatsugu Hirokawa⁴, Shigeaki Kato³

Affiliations

¹ Tokyo University of Agriculture and Technology, Engineering, 2-24-16, Naka-Cho, Koganei, 184-8588, Tokyo, JAPAN.
² Tokyo University of Agriculture and Technology: Tokyo Noko Daigaku, Engineering, JAPAN.
³ Iryo Sosei University: Iryo Sosei Daigaku, Life Science and Engineering, JAPAN.
⁴ University of Tsukuba: Tsukuba Daigaku, Medicine, JAPAN.

PMID: 39843389
DOI: 10.1002/cbic.202401038

Abstract

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 1α,25(OH)2D3. 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.

Keywords: Fluorescent probes; bioorganic chemistry; environmentally responsive fluorescent probe; vitamin D receptor; vitamin D3.