Abstract
Lung cancer, claiming millions of lives annually, has the highest mortality rate worldwide. This advocates the development of novel cancer therapies that are highly toxic for cancer cells but negligibly toxic for healthy cells. One of the effective treatments is targeting overexpressed surface receptors of cancer cells with receptor-specific drugs. The receptors-in-focus in the current review are the G-protein coupled receptors (GPCRs), which are often overexpressed in various types of tumors. The peptide subfamily of GPCRs is the pivot of the current article owing to the high affinity and specificity to and of their cognate peptide ligands, and the proven efficacy of peptide-based therapeutics. The article summarizes various ectopically expressed peptide GPCRs in lung cancer, namely, Cholecystokinin-B/Gastrin receptor, the Bombesin receptor family, Bradykinin B1 and B2 receptors, Arginine vasopressin receptors 1a, 1b and 2, and the Somatostatin receptor type 2. The autocrine growth and pro-proliferative pathways they mediate, and the distinct tumor-inhibitory effects of somatostatin receptors are then discussed. The next section covers how these pathways may be influenced or ‘corrected’ through therapeutics (involving agonists and antagonists) targeting the overexpressed peptide GPCRs. The review proceeds on to Nano-scaled delivery platforms, which enclose chemotherapeutic agents and are decorated with peptide ligands on their external surface, as an effective means of targeting cancer cells. We conclude that targeting these overexpressed peptide GPCRs is potentially evolving as a highly promising form of lung cancer therapy.
Highlights
Lung cancer is a daunting malady victimizing millions globally, on an annual basis
While Cholecystokinin-B/ Gastrin receptor (CCKBR) [24], and Bradykinin receptor 1 (B1R) [264] are not expressed in normal lungs but only in cancerous lungs, all the other receptors included in the present review are expressed in both normal lungs as well as cancerous lungs; they are upregulated in cancerous lungs
The expression of other receptors in normal tissues must be considered when targeting ligands are assessed for use as imaging or therapeutic agents
Summary
Lung cancer is a daunting malady victimizing millions globally, on an annual basis. Being the most common form of tumor worldwide, 1.82 million lung cancer cases were diagnosed and 1.59 million deaths occurred, in 2012 [1]. One of the effective treatments is targeting overexpressed surface receptors of cancer cells with receptorspecific drugs.
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