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As a serine hydrolase synthesized by the liver, butyrylcholinesterase (BChE) is an important biomarker in the clinical diagnosis of liver diseases. To track BChE activity in drug-induced liver injury, we designed a deep-red BChE-activatable fluorescent probe (CYL-BChE) with hemi-cyanine structure by using a cyclopropyl carbonyl group as a specific recognition moiety. Its near-infrared absorption wavelength (665 nm) and emission wavelength (762 nm) provide excellent tissue penetration capabilities, making it suitable for biological imaging.

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Fine-tuning probes for fluorescence polarization binding assays of bivalent ligands against polo-like kinase 1 using full-length protein.

Bioorg Med Chem

December 2024

Chemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, National Institutes of Health, 1050 Boyles St., Frederick, MD 21702, USA.

Polo-like kinase 1 (Plk1) is an important cell cycle regulator that is a recognized target for development of anti-cancer therapeutics. Plk1 is composed of a catalytic kinase domain (KD), a flexible interdomain linker and a polo-box domain (PBD). Intramolecular protein-protein interactions (PPIs) between the PBD and KD result in "auto-inhibition" that is an essential component of proper Plk1 function.

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KRS-1, a biocompatible nickel(II) complex, is introduced as a potent fluorescent probe for PrP fibrillar aggregates. KRS-1 shows a 15-fold enhancement in PL intensity and detects all stages of PrP aggregation. Fluorescence microscopy confirms its efficacy in identifying PrP fibrillar aggregates in HT-22 cells.

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Visualizing Endoplasmic Reticulum Stress and Autophagy in Alzheimer's Model Cells by a Peroxynitrite-Responsive AIEgen Fluorescent Probe.

ACS Chem Neurosci

January 2025

Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, China.

Endoplasmic reticulum (ER) stress and autophagy (ER-phagy) occurring in nerve cells are crucial physiological processes closely associated with Alzheimer's disease (AD). Visualizing the two processes is paramount to advance our understanding of AD pathologies. Among the biomarkers identified, peroxynitrite (ONOO) emerges as a key molecule in the initiation and aggravation of ER stress and ER-phagy, highlighting its significance in the underlying mechanisms of the two processes.

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