LvID-BDP: A Conotoxin-Based Fluorescent Probe for Visualizing α7 nAChR Expression in Intestinal Inflammation

The α7 nicotinic acetylcholine receptor (α7 nAChR) modulates neuroimmune signaling but remains poorly characterized in peripheral disease due to a lack of visualization tools. We developed the fluorescent probe LvID-BDP by conjugating a BODIPY fluorophore to the high-affinity α7 nAChR-targeting peptide LvID. LvID-BDP showed high quantum yield, robust photostability, and sufficient physiological stability for biological imaging. Electrophysiology characterized LvID-BDP as a potent α7 nAChR antagonist, exhibiting a half-maximal inhibitory concentration (IC<sub>50</sub>) of 119.2 nM while retaining high affinity and specificity for the receptor. In murine colon sections, LvID-BDP specifically labeled α7 nAChR, showing strong antibody colocalization (Pearson's <i>R</i> = 0.87) while revealing macrophage-selective enrichment (Pearson's <i>R</i> = 0.85). This probe detected α7 nAChR alterations in engineered and inflamed macrophages and quantified its expression in inflammatory bowel disease (IBD) tissues. LvID-BDP provides a valuable pharmacological tool for specific α7 nAChR visualization in peripheral disease contexts, advancing pathological mechanism research.

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Publication Details

Journal
Journal of Medicinal Chemistry
Published
2026-02-24
DOI
https://doi.org/10.1021/acs.jmedchem.5c03269
Primary Topic
Nicotinic Acetylcholine Receptors Study
Type
article
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article

LvID-BDP: A Conotoxin-Based Fluorescent Probe for Visualizing α7 nAChR Expression in Intestinal Inflammation

dongting zhangsun, Songze Li, Chenxing Xu, Xuetao Zhu et al.
Journal of Medicinal Chemistry
Nicotinic Acetylcholine Receptors Study
article

LvID-BDP: A Conotoxin-Based Fluorescent Probe for Visualizing α7 nAChR Expression in Intestinal Inflammation

dongting zhangsun, Songze Li, Chenxing Xu, Xuetao Zhu, Yao Tan, Tao Ma, Yu Han, Sulan Luo
article en

Abstract

The α7 nicotinic acetylcholine receptor (α7 nAChR) modulates neuroimmune signaling but remains poorly characterized in peripheral disease due to a lack of visualization tools. We developed the fluorescent probe LvID-BDP by conjugating a BODIPY fluorophore to the high-affinity α7 nAChR-targeting peptide LvID. LvID-BDP showed high quantum yield, robust photostability, and sufficient physiological stability for biological imaging. Electrophysiology characterized LvID-BDP as a potent α7 nAChR antagonist, exhibiting a half-maximal inhibitory concentration (IC<sub>50</sub>) of 119.2 nM while retaining high affinity and specificity for the receptor. In murine colon sections, LvID-BDP specifically labeled α7 nAChR, showing strong antibody colocalization (Pearson's <i>R</i> = 0.87) while revealing macrophage-selective enrichment (Pearson's <i>R</i> = 0.85). This probe detected α7 nAChR alterations in engineered and inflamed macrophages and quantified its expression in inflammatory bowel disease (IBD) tissues. LvID-BDP provides a valuable pharmacological tool for specific α7 nAChR visualization in peripheral disease contexts, advancing pathological mechanism research.

Journal of Medicinal ChemistryVol. 69(5)
Guangxi University (CN)
Openalex Percentile: Top 44%
Nicotinic Acetylcholine Receptors Study
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