ACTIVITY-BASED PROTEIN PROFILING (ABPP) BY SMALL MOLECULES LABELING APPROACH

Ph.DDOCTOR OF PHILOSOPH

Microwave-assisted synthesis of 3-acyl-5-hydroxybenzofurans and synthetic studies towar the first total synthesis of ()-N-Deoxymilitarinone A and Militarinone A

127 p.This thesis includes two parts: Microwave-assisted Synthesis of 3-Acyl-5-Hydroxybenzofurans and Synthetic Studies toward the First Total Synthesis of (+)-iV-Deoxymilitarinone A and Militarinone A.​Master of Scienc

A FRET probe with AIEgen as the energy quencher: dual signal turn-on for self-validated caspase detection.

The accurate detection of biological substances is highly desirable to study various biological processes and evaluate disease progression. Herein, we report a self-validated fluorescent probe which is composed of a coumarin fluorophore as the energy donor and a fluorogen with aggregation-induced emission characteristics (AIEgen) as the energy quencher linked through a caspase-3 specific peptide substrate. Unlike the traditionally widely studied fluorescence resonance energy transfer (FRET) probes, our new generation of FRET probe is non-fluorescent itself due to the energy transfer as well as the dissipation of the acceptor energy through the free molecular motion of AIEgen. Upon interaction with caspase-3, the probe displays strong green and red fluorescent signals synchronously due to the separation of the donor-quencher and aggregation of the released AIEgen. The fluorescence turn-on with dual signal amplification allows real-time and self-validated enzyme detection with a high signal-to-background ratio, providing a good opportunity to accurately monitor various biological processes in a real-time manner

Bioorthogonal Turn-On Probe Based on Aggregation-Induced Emission Characteristics for Cancer Cell Imaging and Ablation

10.1002/anie.201601744Angewandte Chemie - International Edition55226457-646

A FRET probe with AIEgen as the energy quencher: dual signal turn-on for self-validated caspase detection

10.1039/c6sc00055jChemical Science774245-425

Multifunctional Liposome: A Bright AIEgen-Lipid Conjugate with Strong Photosensitization

10.1002/anie.201809641Angewandte Chemie - International Edition575016396-1640

Real-Time Specific Light-Up Sensing of Transferrin Receptor: Image-Guided Photodynamic Ablation of Cancer Cells through Controlled Cytomennbrane Disintegration

10.1021/acs.analchem.6b00524ANALYTICAL CHEMISTRY8894841-484

In Situ Proteome Profiling of C75, a Covalent Bioactive Compound with Potential Anticancer Activities

A library of cell-permeable, minimally tagged C75 analogues was synthesized and used to uncover biological targets in human liver cancer cells. Known targets of C75, namely FASN and CPT1A, together with other unknown targets, including PDIA3, TFRC, and GAPDH, were thus identified

Rational Design of a Red-Emissive Fluorophore with AIE and ESIPT Characteristics and Its Application in Light-Up Sensing of Esterase

10.1021/acs.analchem.6b04974Analytical Chemistr8953162-316

Current and Future of “Turn‐On” Based Small‐Molecule Copper Probes for Cuproptosis

Abstract Increasing evidence shows that abnormal copper (Cu) metabolism is highly related to many diseases, such as Alzheimer's disease, Wilson's disease, hematological malignancies and Menkes disease. Very recently, cuproptosis, a Cu‐dependent, programmed cell death was firstly described by Tsvetkov et al. in 2022. Their findings may provide a new perspective for the treatment of related diseases. However, the concrete mechanisms of these diseases, especially cuproptosis, remain completely unclear, the reason of which may be a lack of reliable tools to conduct highly selective, sensitive and high‐resolution imaging of Cu in complex life systems. So far, numerous small‐molecular fluorescent probes have been designed and utilized to explore the Cu signal pathway. Among them, fluorescence turn‐on probes greatly enhance the resolution and accuracy of imaging and may be a promising tool for research of investigation into cuproptosis. This review summarizes the probes developed in the past decade which have the potential to study cuproptosis, focusing on the design strategies, luminescence mechanism and biological‐imaging applications. Besides, we put forward some ideas concerning the design of next‐generation probes for cuproptosis, aiming to tackle the main problems in this new field. Furthermore, the prospect of cuproptosis in the treatment of corresponding diseases is also highlighted