Abstract
Neuropeptide G protein-coupled receptors (GPCRs) are overexpressed on numerous cancer cells. In a number of tumors, such as small cell lung cancer (SCLC), bombesin (BB) like peptides and neurotensin (NTS) function as autocrine growth factors whereby they are secreted from tumor cells, bind to cell surface receptors and stimulate growth. BB-drug conjugates and BB receptor antagonists inhibit the growth of a number of cancers. Vasoactive intestinal peptide (VIP) increases the secretion rate of BB-like peptide and NTS from SCLC leading to increased proliferation. In contrast, somatostatin (SST) inhibits the secretion of autocrine growth factors from neuroendocrine tumors (NETs) and decreases proliferation. SST analogs such as radiolabeled octreotide can be used to localize tumors, is therapeutic for certain cancer patients and has been approved for four different indications in the diagnosis/treatment of NETs. The review will focus on how BB, NTS, VIP, and SST receptors can facilitate the early detection and treatment of cancer.
Highlights
Gprotein-coupled receptors (GPCRs) have 7 transmembrane (T M) domains and they interact with G proteins comprised of α, β, and γ subunits [1]
Most of the research conducted on NTS, BB, and vasoactive intestinal peptide (VIP) has been at the preclinical level
Nonpeptide antagonists are available for the BBR and NTSR which inhibit the proliferation of cancer cells
Summary
Gprotein-coupled receptors (GPCRs) have 7 transmembrane (T M) domains and they interact with G proteins comprised of α, β, and γ subunits [1]. Peptide antagonists such as RC-3095 or (Psi13,14, Leu14)BB blocked the GRPR, and they inhibited the growth of cancer cells [27, 28]. Activation of the NMBR in NSCLC cells causes PI turnover leading to increased phosphorylation of the EGFR (Figure 1).
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