GRPR Membrane Protein Introduction

Introduction of GRPR

Gastrin-releasing peptide receptor (GRPR) is a seven-transmembrane-domain receptor of the GRPR superfamily. It is a mammalian homologue of the amphibian bombesin-like peptide receptor. GRPR is directly coupled to the Gq protein, and GRPR activation leads to an increase in cellular Ca2+ and stimulation of the PLC/PKC and ERK/MAPK pathways. In humans, it is highly expressed in the pancreas and is also expressed in other tissues such as the stomach, adrenal cortex, and brain. Moreover, it is aberrantly expressed in numerous cancers such as those of the lung, colon, and prostate.

Basic Information of GRPR
Protein Name	Gastrin-releasing peptide receptor
Gene Name	GRPR
Aliases	GRP-preferring bombesin receptor
Organism	Homo sapiens (Human)
UniProt ID	P30550
Transmembrane Times	7
Length (aa)	384
Sequence	MALNDCFLLNLEVDHFMHCNISSHSADLPVNDDWSHPGILYVIPAVYGVIILIGLIGNITLIKI FCTVKSMRNVPNLFISSLALGDLLLLITCAPVDASRYLADRWLFGRIGCKLIPFIQLTSVGVSV FTLTALSADRYKAIVRPMDIQASHALMKICLKAAFIWIISMLLAIPEAVFSDLHPFHEESTNQ TFISCAPYPHSNELHPKIHSMASFLVFYVIPLSIISVYYYFIAKNLIQSAYNLPVEGNIHVKKQ IESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLHFVTSICARLLAFTNSCVNP FALYLLSKSFRKQFNTQLLCCQPGLIIRSHSTGRSTTCMTSLKSTNPSVATFSLINGNICHERYV

Functions of GRPR Membrane Protein

By binding to gastrin-releasing peptide (GRP), this receptor mediates different functions of the gastrointestinal and central nervous system, including the release of gastrointestinal hormones, smooth muscle contraction, and epithelial cell proliferation. Since they are distributed throughout the mammalian CNS, evidence has indicated that GRPR might be involved in the neurochemical alterations associated with psychiatric and neurological disorders, supporting that the GRPR should be considered as a therapeutic target for a subset of CNS diseases. Moreover, studies have reported that GRPR may be dedicated to mediating the itch sensation in the dorsal horn of the spinal cord, and thus may provide a central therapeutic target for antipruritic drug development. Additionally, studies have suggested that the GRPR may be potential therapeutic targets for many types of cancer. Moreover, this receptor contributes to the regulation of food intake and fear learning.

Applications of GRPR Membrane Protein in Literature

1. Ma Z., et al. Distribution of the pig gastrin-releasing peptide receptor and the effect of GRP on porcine Leydig cells. Peptides. 2018, 99: 142-152. PubMed ID: 28966141

   This study cloned and analyzed the pig gastrin-releasing peptide receptor (GRPR) cDNA, their expression levels and distribution in pig tissues, as well as the effect of GRP on porcine Leydig cells. The results showed that the CRP/GRPR system might be critical in regulating the reproductive system of the boar.

2. Begum A.A., et al. Bombesin/oligoarginine fusion peptides for gastrin releasing peptide receptor (GRPR) targeted gene delivery. Bioorganic & Medicinal Chemistry. 2018, 26(2):516. PubMed ID: 29269254

   This article reported the development of a peptide-based non-viral gene delivery system: bombesin/oligoarginine and bombesin/oligoarginine/GALA fusion peptide. The efficiency of this delivery system was also evaluated.

3. Popp I., et al. Approaches to improve metabolic stability of a statine-based GRP receptor antagonist. Nuclear Medicine & Biology. 2017, 45:22-29. PubMed ID: 27865999

   This study evaluated the effect of N-terminal modulations of the statine-based GRPR antagonist on its binding affinity, pharmacokinetic properties, and in vivo metabolic stability.

4. Dalm S.U., et al. In vitro and in vivo application of radiolabeled gastrin-releasing peptide receptor ligands in breast cancer. J Nucl Med. 2015, 56(5): 752-7. PubMed ID: 25791989

   This study explored the application of GRPR radioligands for imaging and therapy of breast cancer by using preclinical in vitro and in vivo models. The results showed that GRPR radioligands were promising tools for nuclear imaging and therapy.

5. Roesler R., et al. Gastrin-releasing peptide receptor signaling in the integration of stress and memory. Neurobiology of Learning & Memory. 2014, 112:44-52. PubMed ID: 24001571

   This article reviewed the role of GRP/GRPR system in mediating the stress responses, memory, and fearful events. The results suggested GRPR as an important component in the neurobiological system, in both stress and memory.

GRPR Preparation Options

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