1. Signaling Pathways
  2. GPCR/G Protein
  3. GLP Receptor

GLP Receptor (胰高血糖素样肽受体)

GLP Receptor

GLP 受体包含两个家族成员,GLP-1 受体 (GLP1R 或 GLP-1R) 和 GLP-2 受体 (GLP2R 或 GLP-1R),由胰高血糖素样肽 (GLP) 激活。GLP 由肠细胞分泌;引起胰岛素释放;抑制胰高血糖素分泌、食欲和能量摄入;并延迟胃排空,因为 GLP 受体位于肠道、胰腺、脑干、下丘脑和迷走神经传入神经上。GLP-1 只有一个已知受体 GLP1R,可调节肠道运动、食欲、胰岛功能和葡萄糖稳态,而 GLP2R 的激动剂 GLP-2 可增强肠道营养吸收。GLP-1R 激动剂用于治疗糖尿病和肥胖症,GLP-2R 激动剂被批准用于治疗短肠综合征。对 GLP 受体激活对胆囊运动作用的研究表明,GLP-2 受体激活会增加体内胆囊体积,并降低体外 GBSM 束的自发活动。与通过腺苷酸环化酶-蛋白激酶 A-KATP 通道通路引起作用的抑制性递质一样,GLP-2 受体也通过该通路发出信号。

The GLP receptors contain two family members, GLP-1 receptor (GLP1R, or GLP-1R) and GLP-2 receptor (GLP2R or GLP-1R), activated by the glucagon-like peptides (GLPs). GLPs are s secreted by intestinal cells; causes insulin release; inhibits glucagon secretion, appetite, and energy intake; and delays gastric emptying because GLP receptors are located on the gut, pancreas, brainstem, hypothalamus, and vagal-afferent nerves. GLP-1 has only one known receptor, GLP1R, and regulates gut motility, appetite, islet function, and glucose homeostasis, whereas GLP-2, the agonist of GLP2R, enhances intestinal nutrient absorption. GLP-1R agonists are used to treat diabetes and obesity, and a GLP-2R agonist is approved to treat short bowel syndrome. An investigation of the actions of GLP receptor activation on gallbladder motility has demonstrated that GLP-2 receptor activation increases gallbladder volume in vivo and decreases spontaneous activity in GBSM bundles ex vivo. Like the inhibitory transmitters, which elicit their actions via an adenylate cyclase-protein kinase A-KATP channel pathway, the GLP-2 receptor signals through this same pathway.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P990990
    Efsubaglutide alfa
    Efsubaglutide alfa 是一种靶向 GLP-1 受体的融合蛋白。
    Efsubaglutide alfa
  • HY-P990967
    Sonefpeglutide
    Sonefpeglutide 是一种靶向 GLP1R 的人源抗体。
    Sonefpeglutide
  • HY-164535
    Maridebart cafraglutide Agonist
    Maridebart cafraglutide (AMG 133) 是一种抗体-肽结合物,作为 GLP-1 受体激动剂和 GIP 受体拮抗剂。Maridebart cafraglutide 可以在雄性肥胖小鼠和猕猴中减轻体重并改善代谢指标。Maridebart cafraglutide 有望用于肥胖的研究。
    Maridebart cafraglutide
  • HY-164774
    (4S)-GLP-1 receptor agonist 14 Modulator
    (4S)-GLP-1 receptor agonist 14 (Compound 73) 是一种 GLP-1 受体调节剂。
    (4S)-GLP-1 receptor agonist 14
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