CCKBR Membrane Protein Introduction

Introduction of CCKBR

CCKBR is a type B gastrin receptor that encoded by CCKBR gene. It belongs to the seven-transmembrane domain β-adrenergic receptor superfamily. There are 3 isoforms of the human CCK-BR protein resulted from alternative splicing. It acts as a G-protein coupled receptor for gastrin and cholecystokinin (CCK), which are gut-brain peptides that have regulatory functions in the brain and gastrointestinal tract. CCKBRs are the major population of central CCK receptors and have a high affinity for both sulfated and nonsulfated CCK analogs.

Basic Information of CCKBR
Protein Name Gastrin/cholecystokinin type B receptor
Gene Name CCKBR
Aliases Cholecystokinin-2 receptor, CCK-B receptor, CCK2-R
Organism Homo sapiens (Human)
UniProt ID P32239
Transmembrane Times 7
Length (aa) 516

Function of CCKBR Membrane Protein

CCK is considered to function as neurotransmitters and hormones in two major organ systems: the gastrointestinal tract and the peripheral and central nervous system (CNS). CCK receptors have a significant influence neurotransmission in the brain, regulating anxiety, feeding, and locomotion. This receptor possesses a complex regulation of dopamine activity in the brain. CCKBR exist predominantly in the gastrointestinal tract and the CNS where it can regulate anxiety, analgesia, arousal, and neuroleptic activity. The expression of CCK-B may correlate parallel to anxiety and depression phenotypes in humans. This receptor mediates its action through the association with G proteins that activate a phosphatidylinositol-calcium second messenger system. CCKBR has supposed to be involved in the development of gastro-intestinal cancers and play a modulatory role in Parkinson’s disease.

CCKBR Membrane Protein IntroductionFig.1 Structure of CCKBR membrane protein.

Application of CCKBR Membrane Protein in Literature

1. Plaza A., et al. Cholecystokinin is involved in triglyceride fatty acid uptake by rat adipose tissue. J Endocrinol. 2018, 236(3): 137-150. PubMed ID: 29339381

Authors in this group show that cholecystokinin promotes lipid storage in WAT by acting on adipocyte CCK-2R, suggesting a pivotal role for CCK in TG homeostasis.

2. Smith J.P., et al. Gastrin and Gastric Cancer. Cell Mol Gastroenterol Hepatol. 2017, 4(1): 75-83. PubMed ID: 28560291

Gastrin's actions are mediated through the G-protein-coupled receptor cholecystokinin-B (CCK-B) on parietal and enterochromaffin cells of the gastric body. This article demonstrated that CCK-B signaling pathway has contributed to therapeutic strategies to treat gastric cancer by either targeting the CCK-B receptor with small-molecule antagonists or targeting the peptide with immune-based therapies.

3. Yu B., et al. MiR-148a Functions as a Tumor Suppressor by Targeting CCK-BR via Inactivating STAT3 and Akt in Human Gastric Cancer. PLoS One. 2016, 11(8): e0158961. PubMed ID: 27518872

This article reports that siRNA-induced knockdown of CCKBR elicited similar anti-oncogenic effects (decreased proliferation and migration) as those induced by enforced miR-148a expression.

4. Smith J.P., et al. Distribution of cholecystokinin-B receptor genotype between patients with pancreatic cancer and controls and its impact on survival. Pancreas. 2015, 44(2): 236-42. PubMed ID: 25469546

Cholecystokinin (CCK) and gastrin stimulate the growth of pancreatic cancer through the CCK-B receptor (CCK-BR).This article reveals that the CCK-BR SNP predicts survival and should be studied as a candidate genetic biomarker for those at risk of pancreatic cancer.

CCKBR Preparation Options

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