你把自家产生各种肠道荷尔蒙的农场荒废了,不想通过改变生活习惯和饮食修复,的确可以外购山寨货,GLP-1受体激动剂,到GIP/GLP-1双受体激动剂都上市了,而且顺带一提,双激动剂的副作用更少,少了很多恶心反应(因为GLP-1本来就减慢胃肠道排空,你还想怎样呢?),大概是山寨人体荷尔蒙越是彻底,副作用就更少吧,不久估计会...
GLP-1的促胰岛素分泌作用在β细胞中,GLP-1与其受体结合导致腺苷酸环化酶(AC)的激活,随后导致cAMP增加(图2)[24]。虽然GLP-1(1-37)和GLP-1(7-37)都能刺激胰岛素分泌,但GLP-1(7-37)在低剂量时有效。在5μm剂量下,GLP-1(1-37)和GLP-1(7-37)均可使大鼠胰岛素瘤RIN1046-38细胞内cAMP水平升高,但在5...
与cAMP的增加一样,GLP-1(7-37)对RIN1046-38细胞胰岛素mRNA的刺激也比GLP-1(1-37)更大 [24] ,进一步支持GLP-1(7-37)比GLP-1(1-37)具有更强的促胰岛素分泌作用。cAMP通过环核苷酸磷酸二酯酶3B (PDE3B)过表达来加速cAMP水解,从而减少GLP-1诱导的胰岛素分泌 [25] ,凸显了cAMP在GLP-1促胰岛素分泌方面的...
[21] Gunnarsson, P.T., Winzell, M.S., Deacon, C.F., Larsen, M.O., Jelic, K., Carr, R.D., et al. 2006. Glucose-induced incretin hormone release and inactivation are differently modulated by oral fat an...
[21] Gunnarsson, P.T., Winzell, M.S., Deacon, C.F., Larsen, M.O., Jelic, K., Carr, R.D., et al. 2006. Glucose-induced incretin hormone release and inactivation are differently modulated by oral fat and protein in mice. Endocrinology 147:3173-3180. ...
自胰高糖素样肽-1(GLP-1)被发现以来,它已然成为一种“多面手”激素——其多种代谢功能被人们发现,远远超出了作为肠促胰素的经典定义。GLP-1的众多有益的靶点作用使其受体激动剂逐渐成为更多新兴的治疗领域如脂肪肝、肥胖和神经退行性疾病等的冉冉之“星”药物。时值利拉鲁肽在我国上市10周年,司美格鲁肽新上市之...
PCSK1:激素前转化酶1/3;PCSK2:激素前转化酶2;NTS:孤束核;GRPP:肠高血糖素相关肽;IP-1:中间肽-1;IP-2:中间肽-2;MPGF:主要胰高血糖素原片段;GLP-1:胰高糖素样肽-1;GLP-2:胰高糖素样肽-2。 02 GLP-1刺激胰岛素分泌和合成的分子机制
3. Brubaker PL, Drucker DJ. Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors & Channels, 2011, 8 : 179–188. 4. Francisco Kerr Saraiva , Andrei C Sposito. Cardiovascular effects of Glucagon-like ...
首先,GLP1R激活可上调heat shock protein 90 (HSP90)的表达,减轻心肌细胞凋亡。HSP90是一种分子伴侣蛋白,可以稳定Akt、eNOS等心肌保护蛋白,阻止其降解。研究表明,GLP-1类似物通过诱导HSP90表达,减轻心肌梗死面积[105]。此外,HSP90还可促进SIRT1的表达和活性,而SIRT1可去乙酰化并激活多种抗氧化和抗凋亡分子,如Fox...
[3] Graaf, C.d, Donnelly, D., Wootten, D.,et al. Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes. Pharmacological reviews, 2016, 68(4), 954–1013. [4]Donnelly D. The structure and function of the glucagon-like peptide-1 ...