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Published on: June 18, 2013
The role of HER2 in cancer therapy and targeted drug delivery
Wanyi Tai1, Rubi Mahato, Kun Cheng
1Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 2464 Charlotte Street, Kansas City, MO 64108, USA.
Abstract:
HER2 is highly expressed in a significant proportion of breast cancer, ovarian cancer, and gastric cancer. Since the discovery of its role in tumorigenesis, HER2 has received great attention in cancer research during the past two decades. Successful development of the humanized monoclonal anti-HER2 antibody (Trastuzumab) for the treatment of breast cancer further spurred scientists to develop various HER2 specific antibodies, dimerization inhibitors and kinase inhibitors for cancer therapy. On the other hand, the high expression of HER2 and the accessibility of its extracellular domain make HER2 an ideal target for the targeted delivery of anti-tumor drugs as well as imaging agents. Although there is no natural ligand for HER2, artificial ligands targeting HER2 have been developed and applied in various targeted drug delivery systems. The emphasis of this review is to elucidate the roles of HER2 in cancer therapy and targeted drug delivery. The structure and signal pathway of HER2 will be briefly described. The role of HER2 in tumorigenesis and its relationship with other tumor markers will be discussed. For the HER2 targeted cancer therapy, numerous strategies including the blockage of receptor dimerization, inhibition of the tyrosine kinase activity, and interruption of the downstream signal pathway will be summarized. For the targeted drug delivery to HER2 positive tumor cells, various targeting ligands and their delivery systems will be described in details.
Insights
Human epidermal growth factor receptor 2 (HER2) is a key target in treating HER2-positive cancers like breast and gastric cancer. Research explores HER2-targeted therapies and drug delivery systems for improved treatment outcomes.
Area of Science:
- Oncology
- Molecular Biology
- Biotechnology
Background:
- Human epidermal growth factor receptor 2 (HER2) is overexpressed in breast, ovarian, and gastric cancers, playing a crucial role in tumorigenesis.
- The development of anti-HER2 therapies, such as Trastuzumab, has significantly advanced cancer treatment.
- HER2's high expression and accessible extracellular domain make it a prime target for drug delivery and imaging.
Purpose of the Study:
- To review the roles of HER2 in cancer therapy and targeted drug delivery.
- To discuss HER2's structure, signaling pathways, and involvement in tumorigenesis.
- To summarize current strategies for HER2-targeted cancer therapy and drug delivery systems.
Main Methods:
- Review of scientific literature on HER2 in cancer.
- Analysis of HER2 structure, signaling pathways, and tumorigenic roles.
- Summary of therapeutic strategies targeting HER2, including antibody therapy, dimerization inhibitors, and kinase inhibitors.
- Description of targeted drug delivery systems utilizing HER2 as a target.
Main Results:
- HER2 is a validated target for cancer therapy, with multiple treatment modalities developed.
- Targeted drug delivery systems leveraging HER2 are effective for delivering anti-tumor agents and imaging agents to HER2-positive tumor cells.
- Artificial ligands have been developed for HER2-targeted drug delivery systems.
Conclusions:
- HER2 remains a critical target in oncology, with ongoing advancements in therapeutic strategies.
- Targeted delivery of therapeutics and imaging agents to HER2-positive cancers shows significant promise.
- Further research into HER2-targeted approaches can lead to more effective cancer treatments.
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