2. Academic Validation
  3. Fused Cycloheptatriene-BODIPY Is a High-Performance Near-Infrared Probe to Image Tau Tangles

Fused Cycloheptatriene-BODIPY Is a High-Performance Near-Infrared Probe to Image Tau Tangles

  • J Med Chem. 2022 Nov 10;65(21):14527-14538. doi: 10.1021/acs.jmedchem.2c00859.
Tianxin Xie 1,  Yuying Li 1,  Chuan Tian 1,  Chang Yuan 1,  Bin Dai 2,  Shubo Wang 3,  Kaixiang Zhou 1,  Jiaqi Liu 2,  Hongwei Tan 1,  Yi Liang 2,  Jiapei Dai 4,  Baian Chen 5 3,  Mengchao Cui 1 6
Affiliations

Affiliations

  • 1 Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
  • 2 College of Life Sciences, TaiKang Center for Life and Medical Sciences, Hubei Key Laboratory of Cell Homeostasis, Wuhan University, Wuhan 430072, China.
  • 3 Laboratory Animal Resource Center, Capital Medical University, Beijing 100069, China.
  • 4 Wuhan Institute for Neuroscience and Neuroengineering, South-Central University for Nationalities, Wuhan 430074, China.
  • 5 School of Basic Medical Sciences, Beijing Key Laboratory of Neural Regeneration and Repair, Capital Medical University, Beijing 100069, China.
  • 6 Center for Advanced Materials Research, Beijing Normal University, Zhuhai 519087, China.
PMID: 36283122 DOI: 10.1021/acs.jmedchem.2c00859
Abstract

Neurofibrillary tangles (NFTs), which are composed of abnormally hyperphosphorylated Tau, are one of the main pathologic hallmarks of Alzheimer's disease and Other tauopathies. The fluorescent imaging probes currently used to target NFTs cannot distinguish them well from β-amyloid plaques, thus limiting their utility to diagnose diseases. Here, we developed a fused cycloheptatriene-BODIPY derivative (TNIR7-1A) that displays properties favorable for near-infrared (NIR) imaging with high affinity and specificity to NFTs in vitro. In addition, TNIR7-1A effectively penetrated the blood-brain barrier and clearly distinguished tauopathy in transgenic mice (rTg4510) from control mice using NIR fluorescence imaging in vivo. The sensitivity and specificity of TNIR7-1A for NFTs were confirmed ex vivo by fluorescence staining of the tauopathy mouse model, while molecular docking studies indicated that TNIR7-1A bound to NFTs through hydrophobic interactions. These results suggest that TNIR7-1A can act as a high-performance probe to detect NFTs in vitro and in vivo selectively.

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