Sep 262014

Cancer, Chemistry, and the Cell: Molecules that Interact with the Neurotensin Receptors

R.M. Myers,* J.W. Shearman, M.O. Kitching, A. Ramos-Montoya, D.E. Neal, S.V. Ley, ACS Chem. Biol.2009, 4, 503-525.


The literature covering neurotensin (NT) and its signalling pathways, receptors, and biological profile is complicated by the fact that the discovery of three NT receptor subtypes has come to light only in recent years. Moreover, a lot of this literature explores NT in the context of the central nervous system and behavioral studies. However, there is now good evidence that the up-regulation of NT is intimately involved in cancer development and progression. This Review aims to summarize the isolation, cloning, localization, and binding properties of the accepted receptor subtypes (NTR1, NTR2, and NTR3) and the molecules known to bind at these receptors. The growing role these targets are playing in cancer research is also discussed. We hope this Review will provide a useful overview and a one-stop resource for new researchers engaged in this field at the chemistry−biology interface.


Agonist: A molecule that binds to a specific receptor and triggers a response in the cell mimicking the action of an endogenous ligand.Antagonist: A molecule that binds to a specific receptor yet does not provoke a biological response itself upon binding but blocks or dampens the agonist-mediated response.Homology and identity: Measures of similarity between protein sequences. Homology implies an evolutionary link and is qualitative, whereas identity is quantifiable.Site-directed mutagenesis: A process where specific single nucleotide changes within a gene can be made resulting in the change of a specific amino acid within a protein sequence.Prognostic factor: A biomarker that can be used to estimate the chance of recovery from a disease or the chance of the disease recurring.Predictive factor: A biomarker used to predict the response of a cancer to a given therapy.


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