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Endothelin receptor antagonists as therapeutic agents for cancer
1Abbott Laboratories, Santa Clara, CA 95054, USA. ruth.r.wuwong@abbott.com
Abstract:
Endothelins (ETs) are 21-amino acid peptides involved in many different pathological conditions. ETs, mediated by the ET(A) receptor, are mitogenic for many types of cancer cells. ETs seem to both promote and inhibit apoptosis, dependent on the cell and tissue types. The anti-apoptotic effect of ETs is mediated predominantly by the ET(A) receptor. The ET system also plays a role in metastases. Indeed, animal studies and human clinical trials with ET(A) receptor antagonists suggest that they may be useful therapeutic agents for treating cancer. This paper reviews recent studies on the role of the ET system in tumorigenesis and provides an update on the recent development of ET receptor antagonists, in clinical studies for cancer.
Insights
Endothelins (ETs) are peptides implicated in cancer. ET(A) receptor antagonists show promise as therapeutic agents for treating various cancers, with ongoing clinical studies.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Endothelins (ETs) are peptides involved in numerous pathological conditions.
- ETs, acting via the ET(A) receptor, exhibit mitogenic effects on cancer cells and influence apoptosis.
- The ET system is implicated in cancer progression and metastasis.
Purpose of the Study:
- To review recent studies on the role of the ET system in tumorigenesis.
- To provide an update on the development of ET receptor antagonists for cancer therapy.
Main Methods:
- Review of recent scientific literature.
- Analysis of data from animal studies and human clinical trials.
Main Results:
- ETs, particularly via the ET(A) receptor, promote cancer cell proliferation and affect apoptosis.
- The ET system plays a significant role in cancer metastasis.
- ET(A) receptor antagonists have demonstrated potential as anti-cancer therapeutic agents.
Conclusions:
- The ET system is a critical factor in cancer development and progression.
- ET(A) receptor antagonists represent a promising therapeutic strategy for cancer treatment.
- Further clinical development of ET receptor antagonists is warranted for various cancers.