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|
|Aliases||GRP-preferring bombesin receptor|
|Organism||Homo sapiens (Human)|
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
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.
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.
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.
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.
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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