NK-1 receptor antagonists as antitumor drugs: a survey of the literature from 2000 to 2011.
BACKGROUND
After binding to the neurokinin (NK-1) receptor, substance P (SP) induces tumor cell proliferation, the migration of tumor cells (invasion and metastasis) and angiogenesis. By contrast, NK-1 receptor antagonists inhibit tumor cell proliferation (tumor cells die by apoptosis), block the migratory activity of tumor cells and exert antiangiogenic properties.


METHODS
This review offers a 12-year overview of the underlying mechanism of the action of the SP/NK-1 receptor system and NK-1 receptor antagonists in cancer, providing a new approach to the treatment of tumors.


CONCLUSIONS
Chemically diverse NK-1 receptor antagonists have been identified. The antitumor action of these compounds is independent of their chemical structures and such action is associated with their affinity for the NK-1 receptor and with the dose of the antagonist administered. The NK-1 receptor can be considered as a target in cancer treatment and NK-1 receptor antagonists could be considered as new antitumor drugs. The NK-1 receptor antagonist aprepitant is used in clinical practice and exerts an antitumor action against tumor cells in vitro. In the future, such antitumor action should be tested in human clinical trials.
Hospital Infantil Universitario Virgen del Rocío, Unidad de Cuidados Intensivos Pediátricos, Av. Manuel Siurot s/n, 41013 - Sevilla, Spain. mmunoz@cica.es
Miguel
M
Muñoz
Juan
J
Martinez-Armesto
Rafael
R
Coveñas
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D064729:Neurokinin-1 Receptor Antagonists; D010330:Patents as Topic; D013373:Substance P / Q000378:metabolism
D000970:Antineoplastic Agents; D064729:Neurokinin-1 Receptor Antagonists; D013373:Substance P