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Labeling DNA Probes03:31

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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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Baylis-Hillman Adducts as a Versatile Module for Constructing Fluorogenic Release System.

Lanning Zhao1,2, Yuan Qu3, Fang Zhang1

  • 1State Key Laboratory of Applied Organic Chemistry and College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou 730000, China.

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|April 15, 2022
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This summary is machine-generated.

Researchers developed a versatile thiol-triggered system for controlled molecule release. This fluorogenic system, utilizing Baylis-Hillman adducts, enables rapid, high-yield release and fluorescence enhancement for applications in drug delivery and imaging.

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Area of Science:

  • Chemical Biology
  • Organic Chemistry
  • Biomedical Engineering

Background:

  • Controlled release of molecules of interest (MOI) is crucial for applications like drug delivery and probe design.
  • Existing methods may lack efficiency, speed, or versatility in triggering and release mechanisms.

Purpose of the Study:

  • To develop a novel, versatile, and efficient thiol-triggered fluorogenic release system.
  • To demonstrate the system's utility in prodrug design and in vivo imaging and therapy.

Main Methods:

  • Utilized Baylis-Hillman (BH) adducts as a core module for MOI integration.
  • Developed a thiol-triggered system for rapid and quantitative release of MOI.
  • Synthesized and tested prodrugs for camptothecin and nitric oxide (NO) release.
  • Visualized prodrug activation in live cells and mouse tissues using two-photon microscopy.

Main Results:

  • Achieved fast (∼10 min) and high-yield (>250-fold fluorescence increment) MOI release.
  • Successfully integrated various functional groups (amino, hydroxyl, carboxylic, sulfhydryl) into the BH adduct module.
  • Demonstrated successful in vitro and in vivo visualization of prodrug activation.
  • Validated the therapeutic potential of a NO-releasing prodrug in a stroke model.

Conclusions:

  • The BH adduct-based fluorogenic release system offers a versatile platform for controlled molecule delivery.
  • Advantages include ease of preparation, broad functional group compatibility, rapid response, high yield, and tunable emission.
  • This system shows significant promise for broad applications in chemical biology, drug delivery, and diagnostics.