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Establishment of environment-sensitive probes targeting BRD3/BRD4 for imaging and therapy of tumor
Yuqi Gao1, Jie Zhang2, JianJun Li2
1College of Radiology, Shandong First Medical University, University & Shandong Academy of Medical Sciences, Taian, Shandong, 271016, China; Medical Science and Technology Innovation Center, Shandong First Medical University, Jinan, Shandong, 250117, China.
Abstract:
The BET (bromo and extra-terminal) family proteins are epigenetic readers and master transcription coactivators, which have attracted great interests as cancer therapeutic targets. However, there are few developed labeling toolkits that can be applied for the dynamic studies of BET family proteins in living cells and tissue slices. In order to label and study the distribution of the BET family proteins in tumor cells and tumor tissues, a novel series of environment-sensitive fluorescent probes (6a-6c) were designed and evaluated for their labeling properties. Interestingly, 6a is capable of identifying tumor tissue slices and making a distinction between the tumor and normal tissues. Moreover, it can localize to the nuclear bodies in tumor slices just like BRD3 antibody. In addition, it also played an anti-tumor role through the induction of apoptosis. All these features render 6a may compatible for immunofluorescent studies and future cancer diagnosis, and guide for the discovery of new anticancer drugs.
Insights
Researchers developed novel fluorescent probes to dynamically study BET proteins, crucial epigenetic regulators and cancer targets. Probe 6a effectively labels tumor tissues, distinguishes them from normal tissues, and shows anti-tumor activity, aiding cancer diagnosis and drug discovery.
Area of Science:
- Biochemistry
- Molecular Biology
- Cancer Research
Background:
- BET (bromo and extra-terminal) proteins are key epigenetic readers and transcription coactivators.
- These proteins are significant targets for cancer therapeutics.
- Existing labeling tools for dynamic studies of BET proteins in cells and tissues are limited.
Purpose of the Study:
- To design and evaluate novel environment-sensitive fluorescent probes for labeling BET family proteins.
- To investigate the distribution and properties of these probes in tumor cells and tissues.
- To explore the potential of these probes in cancer diagnosis and drug discovery.
Main Methods:
- Design and synthesis of a series of environment-sensitive fluorescent probes (6a-6c).
- Evaluation of probe labeling properties in living cells and tissue slices.
- Assessment of probe specificity for tumor tissues versus normal tissues.
- Investigation of probe localization within tumor cells (e.g., nuclear bodies).
- Evaluation of the anti-tumor effects of the probes, including apoptosis induction.
Main Results:
- Probe 6a demonstrated effective labeling of BET family proteins.
- Probe 6a could identify tumor tissue slices and differentiate them from normal tissues.
- Probe 6a localized to nuclear bodies in tumor slices, similar to BRD3 antibody.
- Probe 6a exhibited anti-tumor activity by inducing apoptosis.
- The probes showed potential for immunofluorescent studies and cancer diagnosis.
Conclusions:
- Novel fluorescent probes were developed for studying BET family proteins.
- Probe 6a shows promise for distinguishing tumor from normal tissues and has potential therapeutic applications.
- These findings support the use of probe 6a in immunofluorescence, cancer diagnostics, and anticancer drug discovery.
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