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Functional genomics for breast cancer drug target discovery
Tetsuro Yoshimaru1, Yusuke Nakamura2, Toyomasa Katagiri3
1Division of Genome Medicine, Institute of Advanced Medical Sciences, Tokushima University, Tokushima, Japan.
Abstract:
Breast cancer is a heterogeneous disease that develops through a multistep process via the accumulation of genetic/epigenetic alterations in various cancer-related genes. Current treatment options for breast cancer patients include surgery, radiotherapy, and chemotherapy including conventional cytotoxic and molecular-targeted anticancer drugs for each intrinsic subtype, such as endocrine therapy and antihuman epidermal growth factor receptor 2 (HER2) therapy. However, these therapies often fail to prevent recurrence and metastasis due to resistance. Overall, understanding the molecular mechanisms of breast carcinogenesis and progression will help to establish therapeutic modalities to improve treatment. The recent development of comprehensive omics technologies has led to the discovery of driver genes, including oncogenes and tumor-suppressor genes, contributing to the development of molecular-targeted anticancer drugs. Here, we review the development of anticancer drugs targeting cancer-specific functional therapeutic targets, namely, MELK (maternal embryonic leucine zipper kinase), TOPK (T-lymphokine-activated killer cell-originated protein kinase), and BIG3 (brefeldin A-inhibited guanine nucleotide-exchange protein 3), as identified through comprehensive breast cancer transcriptomics.
Insights
New breast cancer drugs target specific genes like MELK, TOPK, and BIG3. These molecularly targeted therapies aim to overcome treatment resistance and improve outcomes for patients with advanced breast cancer.
Area of Science:
- Oncology
- Molecular Biology
- Genetics
Background:
- Breast cancer is a complex, heterogeneous disease driven by genetic and epigenetic changes.
- Current treatments like chemotherapy and targeted therapies (endocrine, anti-HER2) face challenges with recurrence and metastasis due to resistance.
- Understanding molecular mechanisms is crucial for developing improved breast cancer treatments.
Purpose of the Study:
- To review the development of novel anticancer drugs targeting specific molecular targets in breast cancer.
- To highlight the role of omics technologies in identifying new therapeutic targets.
- To focus on MELK, TOPK, and BIG3 as key targets for drug development.
Main Methods:
- Comprehensive analysis of breast cancer transcriptomics data.
- Identification of driver genes and cancer-specific functional targets.
- Review of molecular-targeted anticancer drugs developed against these targets.
Main Results:
- Omics technologies have enabled the discovery of critical driver genes in breast cancer.
- MELK (maternal embryonic leucine zipper kinase), TOPK (T-lymphokine-activated killer cell-originated protein kinase), and BIG3 (brefeldin A-inhibited guanine nucleotide-exchange protein 3) have been identified as promising therapeutic targets.
- Development of anticancer drugs targeting these specific kinases and proteins.
Conclusions:
- Targeting specific molecular pathways like those involving MELK, TOPK, and BIG3 offers a promising strategy to overcome breast cancer resistance.
- Molecularly targeted therapies hold potential for improving treatment efficacy and patient outcomes.
- Continued research into breast cancer genomics and transcriptomics is vital for advancing therapeutic options.
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