4.7 Review

Foundation review: α7-Nicotinic receptor antagonists at the beginning of a clinical era for NSCLC and mesothelioma?

Journal

DRUG DISCOVERY TODAY
Volume 14, Issue 17-18, Pages 822-836

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2009.06.016

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Of the human solid cancers, Non-Small Cell Lung Cancer (NSCLC) and Malignant Pleural Mesothelioma (MPM) display a natural history supporting the concept that they develop from multiple preneoplastic pathways. Recently, new evidence suggested that nicotinic Acetylcholine Receptors (nAChRs) play a significant role in lung cancer predisposition and natural history. This review is based on some translational research aimed at evaluating the potential therapeutic effect of nAChR antagon on NSCLC and MPM. The background and rationale of this approach are based on the experimental observations that: (a) NSCLC and MPM cells express nAChRs and (b) the activation of these receptors by agonists, namely nicotine, inhibits apoptosis, whereas receptor antagonists have a pro-apoptotic effect.

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