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Hyperbranched polyester-based fluorescent probe for histone deacetylase via aggregation-induced emission.

Changmin Yu¹, Yinglong Wu, Fang Zeng

¹College of Materials Science & Engineering, State Key Laboratory of Luminescent Materials & Devices, South China University of Technology , Guangzhou 510640, China.

Biomacromolecules

|November 21, 2013

Summary

This study introduces a novel fluorescent assay for detecting histone deacetylases (HDACs). The assay utilizes a hyperbranched polyester and a TPE derivative, enabling sensitive detection in biological samples.

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Area of Science:

Biochemistry
Analytical Chemistry
Materials Science

Background:

Aberrant histone deacetylase (HDAC) expression is linked to cancer progression and tumor cell proliferation.
Accurate detection of HDAC activity is crucial for cancer diagnostics and therapeutic strategies.
Existing methods for HDAC detection can be complex or lack sensitivity.

Purpose of the Study:

To develop a simple, one-step fluorescent assay for detecting HDAC activity.
To utilize a novel hyperbranched polyester-based system for enhanced sensitivity and applicability.
To establish a reliable method for HDAC detection in biological fluids like serum.

Main Methods:

A one-step fluorescent assay was designed using a hyperbranched polyester functionalized with acetylated lysine (H40-Lys(Ac)).
A negatively charged tetraphenylethylene (TPE) derivative with sulfonic acid groups (TPE-2SO3(-)) was employed as the fluorescent reporter.
HDAC-mediated deacetylation of H40-Lys(Ac) induced electrostatic complexation with TPE-2SO3(-), leading to nanoaggregate formation and fluorescence enhancement via the aggregation-induced emission (AIE) effect.

Main Results:

The assay demonstrated a highly sensitive detection limit for HDAC activity, as low as 25 ng/mL.
The system operates effectively in aqueous media, simplifying experimental procedures.
Successful detection of HDAC activity was achieved in human serum samples, indicating its potential for clinical diagnostics.

Conclusions:

The developed hyperbranched polyester-based fluorescent assay offers a sensitive and efficient method for HDAC detection.
This assay strategy provides a new and effective approach for enzyme activity analysis in biological samples.
The system's simplicity and sensitivity hold promise for advancing cancer diagnostics and research.