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Neurokinin-1 Receptor Antagonists as Anticancer Drugs

[ Vol. 16 , Issue. 10 ]


Miguel Muñoz* and Rafael Coveñas   Pages 1110 - 1129 ( 20 )


Background: Human tumor cells lines and tumor samples overexpress the neurokinin-1 receptor (NK-1R). Substance P (SP), after binding to NK-1Rs, induces tumor cell proliferation, an antiapoptotic effect and promotes angiogenesis and the migration of cancer cells for invasion and metastasis.

Methods: In contrast, NK-1R antagonists block the previous pathophysiological actions mediated by SP. These antagonists promote the death of tumor cells by apoptosis. Peptide and non-peptide NK-1R antagonists have been reported.

Results: Peptide NK-1R antagonists show chemical modifications of the SP molecule (L-amino acids being replaced by D-amino acids), whereas non-peptide NK-1R antagonists include numerous compounds with different chemical compositions while showing similar stereochemical features (affinity for the NK- 1R). Currently, there are more than 300 NK-1R antagonists.

Conclusion: In combination therapy with classic cytostatics, NK-1R antagonists have additive or synergic effects and minimize the side-effects of cytostatics. The effect of NK-1R antagonists as broad-spectrum anticancer drugs is reviewed and the use of these antagonists for the treatment of cancer is suggested.


Angiogenesis, apoptosis, metastasis, NK-1 receptor, substance P, tumor cell.


Research Laboratory on Neuropeptides, Virgen del Rocío University Hospital (IBIS), Sevilla, Laboratory of Neuroanatomy of the Peptidergic Systems, Institute of Neurosciences of Castilla y León (INCYL) University of Salamanca, Salamanca

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