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DNA probes are fragments of DNA labeled with a reporter tag to enable their detection or purification. The resulting labeled DNA probes can then hybridize to target nucleic acid sequences through complementary base-pairing, and may be used to recover or identify these regions.
Radioisotopes, fluorophores, or small molecule binding partners like biotin or digoxigenin, are the most widely used reporter tags for labeling DNA probes. These labels can be attached to the probe DNA molecule via...
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Referential modification strategy based on phenolic hydroxyl-containing KSA luminogens for ER-targeting probe

Qiyun Deng1, Keke Ding2, Yin Li1

  • 1Center for Aggregation-Induced Emission, AIE Institute, State Key Laboratory of Luminescent Materials and Devices, Guangdong Provincial Key Laboratory of Luminescence from Molecular Aggregates, Center for Aggregation-Induced Emission, South China University of Technology, Guangzhou, 510640, PR China.

Biomaterials
|September 13, 2022
PubMed
Summary

Researchers developed new endoplasmic reticulum (ER)-targeting probes using a keto-salicylaldehyde azine (KSA) framework. These probes show promise for cancer theranostics by inducing apoptosis via reactive oxygen species (ROS).

Keywords:
Aggregation-induced emissionEndoplasmic reticulum targetingKeto-salicylaldehyde azinePhenolic hydroxylPhoto-dynamic therapy

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Area of Science:

  • Chemical Biology
  • Molecular Imaging
  • Cancer Theranostics

Background:

  • The endoplasmic reticulum (ER) is crucial for cellular functions and implicated in various diseases.
  • Effective strategies for developing ER-targeting theranostic agents are limited but highly needed for precise treatments.
  • Existing ER-targeting probes lack referential construction methods.

Purpose of the Study:

  • To develop novel ER-targeting luminogens based on the keto-salicylaldehyde azine (KSA) framework.
  • To investigate the theranostic performance of these KSA derivatives for cancer treatment.
  • To establish a reliable strategy for constructing ER-targeting probes.

Main Methods:

  • Synthesis of ER-targeting luminogens based on the KSA framework with introduced phenolic hydroxyl groups.
  • Systematic structural modulation to confirm the role of phenolic hydroxyl groups in ER-targeting.
  • Evaluation of theranostic performance, including selective ER enrichment, luminous efficiency, cellular uptake, ROS generation, and in vitro/in vivo anti-tumor activity.

Main Results:

  • A series of ER-targeting luminogens based on the KSA framework were successfully developed.
  • The phenolic hydroxyl group at the K-terminal was confirmed as key for ER-targeting.
  • Cyanobenzyl moiety at the S-terminal enhanced luminous efficiency and cellular uptake.
  • KSA derivatives generated reactive oxygen species (ROS) to induce ER stress and cancer cell apoptosis, inhibiting tumor growth in vitro and in vivo.

Conclusions:

  • The introduction of a phenolic hydroxyl group to the KSA framework provides a feasible and reliable strategy for developing ER-targeting probes.
  • These KSA derivatives exhibit excellent theranostic performance, enabling precise ER targeting and effective cancer treatment.
  • This approach offers a referential method for the construction of advanced ER-targeting probes for biomedical applications.