Dexamethasone regulation of gastrin-releasing peptide receptor in human lung cells

Novak, John S.; Schleman, Shea; Scott, Joseph; Balderman, Valerie L; Krech, Laura; Kane, Madeleine A.

doi:10.1016/j.lungcan.2003.07.002

Cited by 10 publications

(5 citation statements)

References 40 publications

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“…As shown in Figure , lipopolysaccharide (LPS) (1 μg mL −1 ) induced strong expression of GRPr in RAW264.7 mouse macrophage cells as revealed by immunofluorescence microscopy. The subsequent addition of GRP (0.5 μ m ) transferred the green fluorescence into the cytoplasm, which is consistent with the reported mechanism of GRPr internalization by GRPr agonists . However, pre‐treatment of RAW264.7 cells with complex 8 (1–5 μ m ) blocked GRPr internalization into the cytoplasm (Figure A), indicating that this probe was capable of suppressing GRPr activity in RAW264.7 cells, consistent to what has been reported with other GRPr antagonists .…”

Section: Resultssupporting

confidence: 89%

Peptide‐Conjugated Long‐Lived Theranostic Imaging for Targeting GRPr in Cancer and Immune Cells

Wang

Vellaisamy

et al. 2020

Angewandte Chemie

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Gastrin‐releasing peptide receptor (GRPr) plays proliferative and inflammatory roles in living systems. Here, we report a highly selective GRPr antagonist (JMV594)‐tethered iridium(III) complex for probing GRPr in living cancer cells and immune cells. This probe exhibited desirable photophysical properties and also displayed negligible cytotoxicity, overcoming the inherent toxicity of the iridium(III) complex. Its long emission lifetime enabled its luminescence signal to be readily distinguished from the interfering fluorescence of organic dyes by using a time‐resolved technique. This probe selectively visualized living cancer cells via specific binding to GRPr, while it also modulated the function of GRPr on TNF‐α secretion in immune cells. To our knowledge, this is the first peptide‐conjugated iridium(III) complex developed as a GRPr bioimaging probe and modulator of GRPr activity. This theranostic agent shows great potential at unmasking the diverse roles of GRPr in living systems.

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Section: Resultssupporting

confidence: 89%

Peptide‐Conjugated Long‐Lived Theranostic Imaging for Targeting GRPr in Cancer and Immune Cells

Wang

Vellaisamy

et al. 2020

Angewandte Chemie

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“…Recent studies provide evidence for functional interactions between glucocorticoids and the GRPR system at the cellular level. For instance, dexamethasone exposure significant increased GRPR mRNA and GRPR‐specific binding in human lung cells; moreover, GRPR antagonists blocked dexamethasone‐induced cell proliferation (Novak et al, 2004). Consequently, it is possible that the increased expression of GRPR in amygdala is in part mediated by enhanced adrenocortical function.…”

Section: Discussionmentioning

confidence: 99%

Effect of environmental enrichment on fearful behavior and gastrin‐releasing peptide receptor expression in the amygdala of prenatal stressed rats

Qian

Zhou

Pan

et al. 2008

J of Neuroscience Research

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Prenatal stressed offspring exhibit more fearful behavior in behavioral tests, which can be reversed by environmental enrichment (EE). However, the physiological basis of these phenomena remains unclear. Previous studies revealed that abnormal fearful behavior of prenatally stressed offspring may be a consequence of increased activities of CRFergic systems (corticotropin-releasing factor and its receptors) in the amygdala. Gastrin-releasing peptide receptors (GRPR) also have an important role in regulating amygdala-dependent, fear-related learning. The aim of this study was to examine weather prenatal stress and EE can affect the expression of GRPR in the amygdala. We reported here that prenatal chronic stress (subjected to immobilization and bright light stress for 45 min three times per day) caused increased fearfulness in defensive withdrawal test but had no effect on the expression of GRPR in the amygdala. However, enriched environment housing treatment on postnatal days 21-60 can dramatically increase the expression of GRPR in amygdala and reduce fearfulness in the defensive withdrawal test. Our results demonstrate for the first time that EE can modify the expression of GRPR in the amygdala, which might contribute to our understanding of the physiological effects of environmental enrichment.

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“…However, it is known that the effect of bombesin and related peptides is mediated by three major subtypes of the mammalian bombesin receptors, designated BB 1 (neuromedin B preferring), BB 2 (GRP preferring), and BB 3 (orphan bombesin receptor subtype-3) (13,19). Although the expression of these bombesin receptors on the soma or terminals of pulmonary C-fiber afferents has not been documented, significant levels of GRP specific binding, as well as mRNA as determined by RT-PCR for all three mammalian bombesin receptors, were detected in normal human lung tissue (17,26). All bombesin receptors are known to be G protein-coupled receptors that are coupled via G q/11 to activation of phospholipase C and subsequently activate protein kinase C. The latter has been demonstrated to enhance the neuronal excitability by increasing the phosphorylation of various ion channels such as the TRPV1 (28,37) and TTX-resistance Na ϩ channel (18,29).…”

Section: Discussionmentioning

confidence: 99%

Sensitization of pulmonary chemosensitive neurons by bombesin-like peptides in rats

Gu¹,

Lee²

2005

American Journal of Physiology-Lung Cellular and Molecular Phys

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Small cell lung cancer (SCLC) patients suffer from pulmonary stresses such as dyspnea and chest pain, and the pathogenic mechanisms are not known. SCLC cells secrete a variety of bioactive neuropeptides, including bombesin-like peptides. We hypothesize that these peptides may enhance the sensitivity of the pulmonary chemosensitive nerve endings, contributing to the development of these pulmonary stresses in SCLC patients. This study was therefore carried out to determine the effects of bombesin and gastrin-releasing peptide (GRP), a major bombesin-like peptide, on the sensitivities of pulmonary chemoreflex and isolated pulmonary vagal chemosensitive neurons. In anesthetized, spontaneously breathing rats, intravenous infusion of bombesin or GRP significantly amplified the pulmonary chemoreflex responses to chemical stimulants such as capsaicin and ATP. The enhanced responses were completely abolished by perineural capsaicin treatment of both cervical vagi, suggesting the involvement of pulmonary C-fiber afferents. In isolated pulmonary vagal chemosensitive neurons, pretreatment with bombesin or GRP potentiated the capsaicin-induced Ca(2+) transient. This sensitizing effect was further demonstrated in patch-clamp recording studies; the sensitivities of these neurons to both chemical (capsaicin and ATP) and electrical stimuli were significantly enhanced by the presence of either bombesin or GRP. In summary, our results have demonstrated that bombesin and GRP upregulate the pulmonary chemoreflex sensitivity in vivo and the excitability of isolated pulmonary chemosensitive neurons in vitro.

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Dexamethasone regulation of gastrin-releasing peptide receptor in human lung cells

Cited by 10 publications

References 40 publications

Peptide‐Conjugated Long‐Lived Theranostic Imaging for Targeting GRPr in Cancer and Immune Cells

Peptide‐Conjugated Long‐Lived Theranostic Imaging for Targeting GRPr in Cancer and Immune Cells

Effect of environmental enrichment on fearful behavior and gastrin‐releasing peptide receptor expression in the amygdala of prenatal stressed rats

Sensitization of pulmonary chemosensitive neurons by bombesin-like peptides in rats

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