Hydroxyethyl-Modified Cycloheptatriene-BODIPY Derivatives as Specific Tau Imaging Probes.
Yuying LiChuan TianTianxin XieQi-Lei ZhangJiaqi LiuXiao-Xin YanJiapei DaiYi LiangMeng-Chao CuiPublished in: ACS medicinal chemistry letters (2023)
Near-infrared fluorescence (NIRF) imaging as an exquisite sensitive, high spatial-resolution, and real-time tool plays an important role in visualizing pathologies in the brain. In this study, we designed and synthesized a series of NIR probes of hydroxyethyl cycloheptatriene-BODIPY derivatives that have demonstrated strong binding specificity to native neurofibrillary tangles (NFTs) in Alzheimer's disease (AD) brain sections. The improved hydrophilicity of TNIR7-9 and TNIR7-11 resulted in faster clearance rates from healthy brains (4.2 and 10.9, respectively) compared to previously reported compounds. Furthermore, TNIR7-13 , which features a fluorinated modification, exhibited a high binding affinity to Tau aggregates ( K d = 11.8 nM) and held promise for future PET studies.
Keyphrases
- living cells
- fluorescent probe
- single molecule
- fluorescence imaging
- high resolution
- photodynamic therapy
- resting state
- white matter
- small molecule
- cerebrospinal fluid
- functional connectivity
- computed tomography
- dna binding
- binding protein
- positron emission tomography
- cognitive decline
- pet ct
- big data
- brain injury
- transcription factor
- drug delivery
- mass spectrometry
- mild cognitive impairment
- capillary electrophoresis