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Dual-target Inhibitors Based on BRD4: Novel Therapeutic Approaches for Cancer
Sitao Zhang1, Yanzhao Chen1, Chengsen Tian2
1Department of Medicinal Chemistry, School of Pharmacy, Shandong First Medical University & Shandong Academy of Medical Sciences, Taian 271000, Shandong, China.
Background:
Currently, cancer continues being a dramatically increasing and serious threat to public health. Although many anti-tumor agents have been developed in recent years, the survival rate of patients is not satisfactory. The poor prognosis of cancer patients is closely related to the occurrence of drug resistance. Therefore, it is urgent to develop new strategies for cancer treatment. Multi-target therapies aim to have additive or synergistic effects and reduce the potential for the development of resistance by integrating different pharmacophores into a single drug molecule. Given the fact that majority of diseases are multifactorial in nature, multi-target therapies are being exploited with increasing intensity, which has brought improved outcomes in disease models and obtained several compounds that have entered clinical trials. Thus, it is potential to utilize this strategy for the treatment of BRD4 related cancers. This review focuses on the recent research advances of dual-target inhibitors based on BRD4 in the aspect of anti-tumor.
Methods:
We have searched the recent literatures about BRD4 inhibitors from the online resources and databases, such as pubmed, elsevier and google scholar.
Results:
In the recent years, many efforts have been taken to develop dual-target inhibitors based on BRD4 as anti-cancer agents, such as HDAC/BRD4 dual inhibitors, PLK1/BRD4 dual inhibitors and PI3K/BRD4 dual inhibitors and so on. Most compounds display good anti-tumor activities.
Conclusion:
Developing new anti-cancer agents with new scaffolds and high efficiency is a big challenge for researchers. Dual-target inhibitors based on BRD4 are a class of important bioactive compounds. Making structural modifications on the active dual-target inhibitors according to the corresponding structure-activity relationships is of benefit to obtain more potent anti-cancer leads or clinical drugs. This review will be useful for further development of new dual-target inhibitors based on BRD4 as anti-cancer agents.
Insights
Dual-target inhibitors based on Bromodomain-containing protein 4 (BRD4) show promise for treating cancers. These multi-target therapies integrate different pharmacophores to enhance anti-tumor effects and overcome drug resistance.
Area of Science:
- Oncology
- Medicinal Chemistry
- Pharmacology
Background:
- Cancer remains a significant public health threat with unsatisfactory patient survival rates due to drug resistance.
- Multi-target therapies offer a promising strategy by integrating multiple pharmacophores into a single molecule to enhance efficacy and reduce resistance.
- Bromodomain-containing protein 4 (BRD4) is a potential target for novel anti-cancer drug development.
Purpose of the Study:
- To review recent advances in the development of dual-target inhibitors based on BRD4 for anti-tumor applications.
- To highlight the potential of BRD4-targeted therapies in overcoming cancer drug resistance.
- To provide insights for the future development of potent anti-cancer agents.
Main Methods:
- Comprehensive literature search of BRD4 inhibitors was conducted using online databases (PubMed, Elsevier, Google Scholar).
- Focus on identifying and analyzing dual-target inhibitors incorporating BRD4.
- Review of structure-activity relationships for optimization of anti-cancer leads.
Main Results:
- Several classes of BRD4-based dual-target inhibitors have been developed, including HDAC/BRD4, PLK1/BRD4, and PI3K/BRD4 inhibitors.
- Most investigated compounds demonstrate significant anti-tumor activities in preclinical studies.
- These inhibitors represent a promising approach to combatting cancer.
Conclusions:
- Developing novel, highly effective anti-cancer agents with new scaffolds is a critical challenge.
- BRD4-based dual-target inhibitors are important bioactive compounds with therapeutic potential.
- Further structural modifications guided by structure-activity relationships can lead to more potent clinical drugs.
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