ArticleBritish journal of cancer2005
Expression of V1A and GRP receptors leads to cellular transformation and increased sensitivity to substance-P analogue-induced growth inhibition.
Article in British journal of cancer, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
11 citing papers in PubMed, 25 citations in OpenAlex.
- Butylated Neuropeptide Antagonist Targeting Hypoxia-Induced GRPR Overexpression in Small Cell Lung Cancer.International journal of molecular sciences · 2025Article
- The VJournal of endocrinological investigation · 2022Article
- Article
- Pentapeptides for the treatment of small cell lung cancer: Optimisation by NEuropean journal of medicinal chemistry · 2017Article
- Article
- Is the Canonical RAF/MEK/ERK Signaling Pathway a Therapeutic Target in SCLC?Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer · 2016Review
- Signalling bias in new drug discovery: detection, quantification and therapeutic impact.Nature reviews. Drug discovery · 2013Review
- The potential for selective pharmacological therapies through biased receptor signaling.BMC pharmacology & toxicology · 2012Review
- Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.Pharmacological reviews · 2010Review
- Biased agonism.F1000 biology reports · 2009Article
- Targeting V1A-vasopressin receptors with [Arg6, D-Trp7,9, NmePhe8]-substance P (6-11) identifies a strategy to develop novel anti-cancer therapies.British journal of pharmacology · 2009Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
Abstract
Small-cell lung cancer (SCLC) is a particularly aggressive cancer, which metastasises early. Despite initial sensitivity to radio- and chemo-therapy, it invariably relapses, so that the 2-year survival remains less than 5%. Neuropeptides particularly arginine vasopressin (AVP) and gastrin-releasing peptide (GRP) act as autocrine and paracrine growth factors and the expression of these and their receptors are a hallmark of the disease. Substance-P analogues including [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-substance-P (SP-D) and [Arg6,D-Trp7,9,NmePhe8]-substance-P (6-11) (SP-G) inhibit the growth of SCLC cells by modulating neuropeptide signalling. We show that GRP and V1A receptors expression leads to the development of a transformed phenotype. Addition of neuropeptide provides some protection from etoposide-induced cytotoxicity. Receptor expression also leads to an increased sensitivity to substance-P analogue-induced growth inhibition. We show that SP-D and SP-G act as biased agonists at GRP and V1A receptors causing blockade of Gq-mediated Ca2+ release while directing signalling to activate ERK via a pertussis toxin-sensitive pathway. This is the first description of biased agonism at V1A receptors. This unique pharmacology governs the antiproliferative properties of these agents and highlights their potential therapeutic potential for the treatment of SCLC and particularly in tumours, which have developed resistance to chemotherapy.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.