Bioorthogonal In Situ Formation of AIE Luminogens for Imaging Disease Progression via Sigmoidal Signal Amplification

X Xinyu Yu (Future Battery Research Center, Global Institute of Future Technology) X Xirui Liu (Ningbo Institute of Materials Technology and Engineering) H Hongbao Sun (Department of Radiology and Huaxi MR Research Center (HMRRC), Frontiers Science Center for Disease‐Related Molecular Network, State Key Laboratory of Biotherapy West China Hospital, Sichuan University Huaxi Research Building, 001 4th Keyuan Road Chengdu 610041 China) T Tianruo Shen (National Supercomputer Center in Tianjin) Y Yingqiao Deng (Department of Radiology and Huaxi MR Research Center (HMRRC), Frontiers Science Center for Disease‐Related Molecular Network, State Key Laboratory of Biotherapy West China Hospital, Sichuan University Huaxi Research Building, 001 4th Keyuan Road Chengdu 610041 China) H Haiyan Ren P Peixuan Zou (Department of Biopharmaceutics West China School of Pharmacy, Sichuan University No. 17 People's South Road Chengdu 610041 China) Y Yongxiang Zheng (Department of Biopharmaceutics West China School of Pharmacy, Sichuan University No. 17 People's South Road Chengdu 610041 China) P Peihong Xiao (Department of Laboratory Medicine and Sichuan Provincial Key Laboratory for Human Disease Gene Study, Sichuan Provincial People's Hospital, School of Medicine University of Electronic Science and Technology of China 32 West Section 2, First Ring Road Chengdu 610072 China) Q Qiyong Gong (Department of Radiology, Huaxi MR Research Center, Institute of Radiology and Medical Imaging, West China Hospital of Sichuan University) M Meng Qin X Xiaogang Liu H Haoxing Wu (Department of Radiology and Huaxi MR Research Center (HMRRC), Frontiers Science Center for Disease‐Related Molecular Network, State Key Laboratory of Biotherapy West China Hospital, Sichuan University Huaxi Research Building, 001 4th Keyuan Road Chengdu 610041 China)

Abstract

AbstractAggregation‐induced emission (AIE) luminogens are promising tools for biological imaging, yet their utility is often limited by nonspecific aggregation and elevated background fluorescence. Here, we present a bioorthogonal in situ formation strategy that enables precise, organelle‐specific activation of AIEgens within live cells. This system employs a dual‐lock mechanism—combining tetrazine quenching and twisted intramolecular charge shuttle (TICS) dynamics—to maintain an ultra‐low fluorescence background in the precursor state, even under aggregating conditions. Upon bioorthogonal reactions and molecular aggregation, the resulting AIEgens exhibit tunable emission peaks ranging from 605 to 665 nm, large Stokes shifts (up to 201 nm), and an exceptional fluorescence enhancement (up to 1033‐fold). Their high biocompatibility and spatial precision allow for multiplexed, simultaneous labeling of intracellular targets. Compared to conventional fluorogenic and bioorthogonal probes, these AIEgens exhibit a sigmoidal amplification response, enabling the sensitive discrimination of subtle biomarker expression differences and the effective identification of injured cells during disease progression. This strategy significantly enhances the specificity and sensitivity of live‐cell imaging, expands the functional utility of AIE luminogens, and offers a versatile platform for high‐resolution, multiplexed bioimaging in biomedical research and diagnostics.

Article Details

Volume / Issue Vol. 64, Issue 40
Published September 26, 2025
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (13)

X

Xinyu Yu

Future Battery Research Center, Global Institute of Future Technology

X

Xirui Liu

Ningbo Institute of Materials Technology and Engineering

H

Hongbao Sun

Department of Radiology and Huaxi MR Research Center (HMRRC), Frontiers Science Center for Disease‐Related Molecular Network, State Key Laboratory of Biotherapy West China Hospital, Sichuan University Huaxi Research Building, 001 4th Keyuan Road Chengdu 610041 China

T

Tianruo Shen

National Supercomputer Center in Tianjin

Y

Yingqiao Deng

Department of Radiology and Huaxi MR Research Center (HMRRC), Frontiers Science Center for Disease‐Related Molecular Network, State Key Laboratory of Biotherapy West China Hospital, Sichuan University Huaxi Research Building, 001 4th Keyuan Road Chengdu 610041 China

H

Haiyan Ren

P

Peixuan Zou

Department of Biopharmaceutics West China School of Pharmacy, Sichuan University No. 17 People's South Road Chengdu 610041 China

Y

Yongxiang Zheng

Department of Biopharmaceutics West China School of Pharmacy, Sichuan University No. 17 People's South Road Chengdu 610041 China

P

Peihong Xiao

Department of Laboratory Medicine and Sichuan Provincial Key Laboratory for Human Disease Gene Study, Sichuan Provincial People's Hospital, School of Medicine University of Electronic Science and Technology of China 32 West Section 2, First Ring Road Chengdu 610072 China

Q

Qiyong Gong

Department of Radiology, Huaxi MR Research Center, Institute of Radiology and Medical Imaging, West China Hospital of Sichuan University

M

Meng Qin

X

Xiaogang Liu

H

Haoxing Wu

Department of Radiology and Huaxi MR Research Center (HMRRC), Frontiers Science Center for Disease‐Related Molecular Network, State Key Laboratory of Biotherapy West China Hospital, Sichuan University Huaxi Research Building, 001 4th Keyuan Road Chengdu 610041 China