Recent insights into biological functions of mammalian bombesin-like peptides and their receptors

Qu, Xiangping; Wang, Hui; Liu, Rujiao

doi:10.1097/med.0000000000000375

Cited by 9 publications

(7 citation statements)

References 41 publications

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“…The family of mammalian bombesin receptors is composed of three receptors: Gastrin-releasing peptide receptor (GRP-R/BB2), neuromedin B receptor (NMB-R/BB1), and the orphan bombesin receptor subtype-3 (BRS-3/BB-3) [1]. These mammalian bombesin receptors are specific G-protein-coupled receptors that mediate the diverse actions of bombesin-like peptides (BLPs) in autocrine, paracrine, or neuroendocrine systems [2]. BLPs, including gastrin-releasing peptide (GRP) and neuromedin B (NMB), have been identified in mammalian tissues.…”

Section: Introductionmentioning

confidence: 99%

Involvement of Gastrin-Releasing Peptide Receptor in the Regulation of Adipocyte Differentiation in 3T3-L1 Cells

Park

Kim

Bae

et al. 2018

IJMS

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Gastrin-releasing peptide (GRP), a member of bombesin-like peptides, and its receptor (GRP-R) play an important role in various physiological and pathological conditions. In this work, we investigated the role of GRP-R on adipogenesis in 3T3-L1 adipocytes. The expression of GRP-R was significantly increased during the adipocyte differentiation of 3T3-L1 cells. The inhibition of GRP-R by the antagonist RC-3095 affected adipogenesis in 3T3-L1 cells, which reduced lipid accumulation and regulated the expression of adipogenic genes. Moreover, cyclic AMP response element-binding protein (CREB) directly bound to the GRP-R promoter upon exposure to adipogenic stimuli. The down-regulation of GRP-R by the knockdown of CREB inhibited adipocyte differentiation of 3T3-L1 cells. Together these results suggest that the regulation of GRP-R activity or expression has an influence on adipogenesis through regulating adipogenic related genes.

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Section: Introductionmentioning

confidence: 99%

Involvement of Gastrin-Releasing Peptide Receptor in the Regulation of Adipocyte Differentiation in 3T3-L1 Cells

Park

Kim

Bae

et al. 2018

IJMS

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“…Activation of GRPR and NMBR results in a wide range of physiological/pathophysiological actions, including the stimulation of smooth-muscle contraction (particularly urogenital and gastrointestinal tract), gastrointestinal motility, as a modulator of immune function (stimulate phagocytosis, chemo-attraction of monocytes, macrophages, neutrophils; stimulate macrophage IL-1 release); secretion [pancreatic, gastric, intestinal, endocrine (insulin)], hormone secretion (release of LH, GnRH, prolactin, growth hormone, TSH, CCK, GLP1, enteroglucagon, GIP, PP, neurotensin), and stimulation of a wide range of CNS effects (feeding, behavioral effects, body temperature control, regulation of circadian rhythm, sighing) and functioning as an important spinal neurotransmitter mediating pruritus (12,106,(114)(115)(116)(117)(118)(119)(120). A physiological role for the BRS-3 receptor has yet to be completely defined; however, recently studies suggest an important role in metabolic homeostasis, in glucose and insulin regulation, in obesity and diabetes mellitus, in the regulation of body temperature, and in feeding behavior (14,44,68,(121)(122)(123).…”

Section: Bn/bnr: Physiological/pathophysiological Effectsmentioning

confidence: 99%

Bombesin Receptor Family Activation and CNS/Neural Tumors: Review of Evidence Supporting Possible Role for Novel Targeted Therapy

et al. 2021

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G-protein-coupled receptors (GPCRs) are increasingly being considered as possible therapeutic targets in cancers. Activation of GPCR on tumors can have prominent growth effects, and GPCRs are frequently over-/ectopically expressed on tumors and thus can be used for targeted therapy. CNS/neural tumors are receiving increasing attention using this approach. Gliomas are the most frequent primary malignant brain/CNS tumor with glioblastoma having a 10-year survival <1%; neuroblastomas are the most common extracranial solid tumor in children with long-term survival<40%, and medulloblastomas are less common, but one subgroup has a 5-year survival <60%. Thus, there is an increased need for more effective treatments of these tumors. The Bombesin-receptor family (BnRs) is one of the GPCRs that are most frequently over/ectopically expressed by common tumors and is receiving particular attention as a possible therapeutic target in several tumors, particularly in prostate, breast, and lung cancer. We review in this paper evidence suggesting why a similar approach in some CNS/neural tumors (gliomas, neuroblastomas, medulloblastomas) should also be considered.

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“…GRPR is also expressed in HER2-positive cells. GRPR belongs to the mammalian bombesin (BBN)-like peptide receptor family (Qu et al, 2018). BBN is a 14-amino acid peptide, originally found in the frog skin (Erspamer et al, 1970;Jensen et al, 2008).…”

Section: Other Targets In Her2-positive Models Grprmentioning

confidence: 99%

“…BBN is a 14-amino acid peptide, originally found in the frog skin (Erspamer et al, 1970;Jensen et al, 2008). One of its mammalian homologs is a gastrin-releasing peptide (GRP) (Qu et al, 2018), which binds specifically to GRPR. RM26 (D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2), an antagonist analog of BBN, was conjugated to different lengths of polyethylene glycol (PEG x ) and the NOTA chelator for radiolabeling with 68 Ga to obtain 68 Ga-NOTA-PEG x -RM26 (Peptides, Figure 2) to optimize the radiotracer's targeting efficiency (Varasteh et al, 2014).…”

Section: Other Targets In Her2-positive Models Grprmentioning

confidence: 99%

Preclinical Advances in Theranostics for the Different Molecular Subtypes of Breast Cancer

Fang

Cavaliere

et al. 2021

Front. Pharmacol.

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Breast cancer is the most common cancer in women worldwide. The heterogeneity of breast cancer and drug resistance to therapies make the diagnosis and treatment difficult. Molecular imaging methods with positron emission tomography (PET) and single-photon emission tomography (SPECT) provide useful tools to diagnose, predict, and monitor the response of therapy, contributing to precision medicine for breast cancer patients. Recently, many efforts have been made to find new targets for breast cancer therapy to overcome resistance to standard of care treatments, giving rise to new therapeutic agents to offer more options for patients with breast cancer. The combination of diagnostic and therapeutic strategies forms the foundation of theranostics. Some of these theranostic agents exhibit high potential to be translated to clinic. In this review, we highlight the most recent advances in theranostics of the different molecular subtypes of breast cancer in preclinical studies.

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Recent insights into biological functions of mammalian bombesin-like peptides and their receptors

Cited by 9 publications

References 41 publications

Involvement of Gastrin-Releasing Peptide Receptor in the Regulation of Adipocyte Differentiation in 3T3-L1 Cells

Involvement of Gastrin-Releasing Peptide Receptor in the Regulation of Adipocyte Differentiation in 3T3-L1 Cells

Bombesin Receptor Family Activation and CNS/Neural Tumors: Review of Evidence Supporting Possible Role for Novel Targeted Therapy

Preclinical Advances in Theranostics for the Different Molecular Subtypes of Breast Cancer

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