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Updated: Oct 4, 2025

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog
Published on: November 5, 2014
Recent progress of palmitoyl transferase DHHC3 as a novel antitumor target
Tian Gao1, Shuya Liu1, Xiaocun Li1
1Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, 071002, China.
Abstract:
DHHC3 is a DHHC-family palmitoyl acyltransferase that is responsible for many mammalian palmitoylation events. By regulating the posttranslational modification of its specific substrates, DHHC3 has shown a strong protumor effect in various cancers. In this review, the authors introduce the research progress of DHHC3 as a new antitumor target through the expression of DHHC3 in patients with tumors, substrate proteins and potential mechanisms. Recent advances in the search for protein structures and inhibitors are also reviewed. Several design strategies to facilitate the optimization of the process of drug design based on DHHC3 are also discussed.
Insights
DHHC3, an enzyme regulating protein modification, shows a tumor-promoting role in cancers. Targeting DHHC3 presents a promising new strategy for developing novel antitumor drugs and therapies.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- DHHC3 is a palmitoyl acyltransferase crucial for mammalian palmitoylation.
- DHHC3 exhibits a significant protumorigenic effect across various cancer types by modifying substrate proteins.
- Dysregulation of DHHC3 contributes to cancer progression.
Purpose of the Study:
- To review the research progress on DHHC3 as a potential antitumor target.
- To explore the expression patterns of DHHC3 in tumors, its substrate proteins, and underlying mechanisms.
- To discuss recent advancements in identifying DHHC3 protein structures and inhibitors for drug design.
Main Methods:
- Literature review of studies on DHHC3 expression, substrates, and mechanisms in cancer.
- Analysis of recent findings on DHHC3 protein structure determination.
- Review of current inhibitor development strategies for DHHC3.
Main Results:
- DHHC3 expression is elevated in tumors, correlating with its protumorigenic activity.
- Specific substrate proteins and their modification by DHHC3 are identified, elucidating its oncogenic pathways.
- Advances in structural biology have provided insights for rational drug design targeting DHHC3.
Conclusions:
- DHHC3 represents a viable and novel target for anticancer drug development.
- Understanding DHHC3's role in posttranslational modification is key to exploiting it as an antitumor strategy.
- Further research into DHHC3 inhibitors and structural biology will accelerate the development of targeted cancer therapies.
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