GRPR(胃泌素释放肽受体)是一种G蛋白偶联受体(GPCR),属于蛙皮素受体亚家族(Bombesin receptor family),该家族还包括NMBR(神经介素B受体)和BRS3(蛙皮素受体亚型3)。GRPR主要通过与配体胃泌素释放肽(GRP)结合激活下游信号通路,参与多种生理功能,如神经传递、平滑肌收缩、细胞增殖和炎症反应。GRPR在神经系统、胃肠道和肺部高表达,尤其在脊髓背角参与痛觉传递,并在某些肿瘤(如前列腺癌、肺癌和乳腺癌)中异常高表达,促进肿瘤生长和转移。GRPR的突变可能导致信号传导异常,例如某些错义突变会降低受体与GRP的亲和力,影响细胞增殖调控,与神经发育障碍或肿瘤发生相关。若GRPR过表达,可能加剧肿瘤的侵袭性和转移潜力,同时激活MAPK和PI3K/AKT等促生存通路;而降低表达或敲除GRPR可抑制肿瘤进展,但可能影响胃肠动力或神经调节功能。GRPR拮抗剂(如RC-3095)正在研究用于癌症治疗。该基因家族的共性是通过结合蛙皮素样肽(如GRP、NMB)激活Gq蛋白,触发钙离子动员和PKC通路,调控细胞生长和分化。此外,GRPR与哮喘和慢性瘙痒等疾病相关,因其在炎症和感觉神经元中的激活作用。
Gastrin-releasing peptide (GRP) regulates numerous functions of the gastrointestinal and central nervous systems, including release of gastrointestinal hormones, smooth muscle cell contraction, and epithelial cell proliferation and is a potent mitogen for neoplastic tissues. The effects of GRP are mediated through the gastrin-releasing peptide receptor. This receptor is a glycosylated, 7-transmembrane G-protein coupled receptor that activates the phospholipase C signaling pathway. The receptor is aberrantly expressed in numerous cancers such as those of the lung, colon, and prostate. An individual with autism and multiple exostoses was found to have a balanced translocation between chromosome 8 and a chromosome X breakpoint located within the gastrin-releasing peptide receptor gene. [provided by RefSeq, Jul 2008]
胃泌素释放肽(GRP)调节消化道和中枢神经系统,包括胃肠激素的释放,平滑肌细胞收缩和上皮细胞增殖的许多功能,并且是肿瘤组织的有力有丝分裂原。 GRP的效果通过胃泌素释放肽受体介导的。该受体是一种糖基化,7-跨膜G蛋白偶联受体激活的磷脂酶C信号传导途径。该受体在许多癌症中异常表达如肺癌,结肠癌,和前列腺癌。患有自闭症和多发性外生骨疣的个体被发现有染色体8和位于所述胃泌素释放肽受体基因内的X染色体断点之间的平衡易位。 [由RefSeq的,2008年7月提供]
GRPR基因(以及对应的蛋白质)的细胞分布位置:
GRPR基因的本体(GO)信息:
名称 |
---|
4020 Calcium signaling pathway [PATH:hsa04020] |
4080 Neuroactive ligand-receptor interaction [PATH:hsa04080] |
名称 |
---|
Class A/1 (Rhodopsin-like receptors) |
G alpha (q) signalling events |
Gastrin-CREB signalling pathway via PKC and MAPK |
GPCR downstream signaling |
GPCR ligand binding |
Peptide ligand-binding receptors |
Signal Transduction |
Signaling by GPCR |
疾病名称 | 关系值 | NofPmids | NofSnps | 来源 |
Prostatic Neoplasms | 0.123267234 | 4 | 0 | BeFree_CTD_human_LHGDN |
Memory Disorders | 0.12 | 1 | 0 | CTD_human |
Small cell carcinoma of lung | 0.006534468 | 5 | 0 | BeFree_LHGDN |
Panic Disorder | 0.005276948 | 2 | 0 | BeFree_GAD |
Autistic Disorder | 0.003452799 | 4 | 1 | BeFree_GAD |
Malignant neoplasm of lung | 0.003181358 | 4 | 0 | BeFree_GAD |
Uterine Neoplasms | 0.00272435 | 1 | 0 | LHGDN |
Duodenal Neoplasms | 0.00272435 | 1 | 0 | LHGDN |
Lung Neoplasms | 0.00272435 | 1 | 0 | LHGDN |
Colonic Neoplasms | 0.00272435 | 1 | 0 | LHGDN |
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