Endothelin receptor antagonists as therapeutic agents for cancer.
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.
Wu-Wong
J Ruth
JR
Abbott Laboratories, Santa Clara, CA 95054, USA. ruth.r.wuwong@abbott.com
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D002986:Clinical Trials as Topic; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000502:physiology; D006801:Humans; D009362:Neoplasm Metastasis / Q000473:pathology; D009369:Neoplasms / Q000188:drug therapy*; D017466:Receptors, Endothelin / Q000502:physiology
D000970:Antineoplastic Agents; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D017466:Receptors, Endothelin