[79] Shu, L., Matveyenko, A.V., Kerr-Conte, J., Cho, J.H., McIntosh, C.H., Maedler, K. 2009. Decreased TCF7L2 protein levels in type 2 diabetes mellitus correlate with downregulation of GIP- and GLP-1 receptors and impaired beta-cell function. Hum Mol Genet 18:2388- 2399. ...
[79] Shu, L., Matveyenko, A.V., Kerr-Conte, J., Cho, J.H., McIntosh, C.H., Maedler, K. 2009. Decreased TCF7L2 protein levels in type 2 diabetes mellitus correlate with downregulation of GIP- and GLP-1 receptors and...
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[79] Shu, L., Matveyenko, A.V., Kerr-Conte, J., Cho, J.H., McIntosh, C.H., Maedler, K. 2009. Decreased TCF7L2 protein levels in type 2 diabetes mellitus correlate with downregulation of GIP- and GLP-1 receptors and impaired beta-cell function. Hum Mol Genet 18:2388- 2399. ...
健康志愿者进行GLP-1输注可快速增加腹部皮下脂肪组织和骨骼肌的血流量,而不改变内脏的血流量[42]。值得注意的是,与GIP相比[43-46],GLP-1诱导的脂肪组织血流量增加并不依赖于餐后高血糖和高胰岛素血症,即使在空腹状态下也可以观察到[42]。 GLP-1R激动剂也被证实可降低T2DM患者的BP[7,18,41]。值得注意的是...
健康志愿者进行GLP-1输注可快速增加腹部皮下脂肪组织和骨骼肌的血流量,而不改变内脏的血流量[42]。值得注意的是,与GIP相比[43-46],GLP-1诱导的脂肪组织血流量增加并不依赖于餐后高血糖和高胰岛素血症,即使在空腹状态下也可以观察到...
2022年2月25日,中国科学院上海药物研究所王明伟/杨德华团队携手徐华强团队在Nature Communications上发表了题为Structural insights into multiplexed pharmacological actions of tirzepatide and peptide 20 at the GIP, GLP-1 or glucagon receptors的研究论文,首次报道了Tirzepatide–GIPR–Gs (3.4 Å)、未酰化Tirzep...
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 ...
总的来说,将GIP活性整合到双重GLP-1/GCG 受体激动中可改善体重减轻和血糖控制,同时缓冲慢性 GCG 受体激动的糖尿病风险。 SAR441255基于选择性GLP-1R激动剂exendin-4结构进行设计,且经过体外测试对GLP-1、GCG和GIP受体的最大活性类似于每个受体的同源内源激动剂。
GIP调节GLP-1的分泌需要通过迷走神经传入或传出信号传输[61]。在人体中,当十二指肠葡萄糖输送速率超过其吸收限度,即未吸收的葡萄糖到达空肠或其他地方,GLP-1才会受到强烈刺激反应性分泌。相反,GIP分泌则可以是由极低的胃葡萄糖递送率刺激,因此近端肠中K-细胞产生GIP的丰度比L-细胞产生的GLP-1更高[62]。