Tailoring obeticholic acid activity by iridium(III) complex conjugation to develop a farnesoid X receptor probe.

ABSTRACT:

Introduction

The farnesoid X receptor (FXR) is a crucial regulator in the intestine, maintaining bile acid homeostasis. Inhibiting intestinal FXR shows promise in managing inflammatory bowel and liver diseases by reducing bile acid accumulation. Additionally, changes in FXR expression could serve as a potential biomarker for intestinal diseases. Therefore, developing an imaging probe for FXR holds significant potential for the early detection, simultaneous treatment, and monitoring of FXR-related diseases.

Objectives

The study aimed to develop a bioimaging probe for FXR by conjugating obeticholic acid (OCA), an FXR agonist, to an iridium(III) complex, and to investigate its application for targeting FXR in intestinal cells.

Methods

OCA was conjugated to an iridium(III

SUBMITTER: Niu D 

PROVIDER: S-EPMC12126729 | biostudies-literature | 2025 May

REPOSITORIES: biostudies-literature