Endothelin receptor antagonists as therapeutic agents for cancer
Wu-Wong, J.R.
Current Opinion in Investigational Drugs 3(8): 1234-1239
2002
ISSN/ISBN: 1472-4472 PMID: 12211422 Document Number: 548168
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.