[12] HU, Zhong-ping, et al. "Research Progress on Structure and Function of GLP-1R and Screening for Small Molecule Drugs." Biotechnology Bulletin 33.2 (2017): 30.[13] Meurot, C., et al. "Targeting the GLP-1/GLP-1R axis to treat osteoarthritis: A new opportunity?." Journal of O...
Figure 1. The structure of GLP1R [4]2、GLP1R分布与功能 GLP-1R 广泛分布在胰腺、胃、十二指肠、肺、心脏、肾脏和脑等许多组织和器官中，但主要是在胰岛β细胞中表达，脑中GLP-1r 密度最高的是孤束核、后区、脚间核、后背核和腹侧被盖核、下丘脑核、丘脑核、伏隔核和侧隔[5]。GLP1R可通过与GLP1及...
[12] HU, Zhong-ping, et al. "Research Progress on Structure and Function of GLP-1R and Screening for Small Molecule Drugs." Biotechnology Bulletin 33.2 (2017): 30. [13] Meurot, C., et al. "Targeting the GLP-1/GLP-1R axis to treat osteoarthritis: A new opportunity?." Journal of O...
参考:G protein-coupled receptors: structure- and function-based drug discovery, Signal Transduct Target Ther. 2021 Jan 8;6(1):7;GLP-1R 结构和功能及小分子药物筛选研究进展,生物技术通报(2017);Structural insights into the activation of GLP-1R by a small molecule agonist, Cell Research (2020) 0...
参考文献 1 Yang, D. et al. G protein-coupled receptors: structure- and function-based drug discovery. Signal Transduct Target Ther 6, 7, doi:10.1038/s41392-020-00435-w (2021).2 Cong, Z. et al. Structural perspective of class B1 GPCR signaling. Trends Pharmacol Sci 43, 321-334...
1 Yang, D. et al. G protein-coupled receptors: structure- and function-based drug discovery. Signal Transduct Target Ther 6, 7, doi:10.1038/s41392-020-00435-w (2021). 2 Cong, Z. et al. Structural perspective of ...
12月18日,硕迪生物(Structure Therapeutics )公布了其小分子GLP-1受体激动剂GSBR-1290治疗2型糖尿病(T2DM)与肥胖症的IIa期研究最新数据。这项随机、双盲、为期12周、安慰剂对照IIa期临床试验迄今为止招募了94例受试者,其中60例受试者随机接受了GSBR-1290。T2DM队列(n
Structure Therapeutics)宣布其高选择性口服胰高血糖素样肽-1(GLP-1)受体激动剂GSBR-1290,在超重或肥胖的健康个体中的进行的1b期多剂量递增(MAD)临床试验中获得积极结果。在为期28天的研究中,最高剂量的GSBR-1290让参与者体重减轻4.9公斤,支持每日一次给药,并具有令人鼓舞的安全性和耐受性特征。
胰岛B细胞中GLP-1R调控的信号通路 参考:Gprotein-coupled receptors: structure- and function-based drugdiscovery, Signal Transduct Target Ther. 2021 Jan 8;6(1):7;GLP-1R结构和功能及小分子药物筛选研究进展,生物技术通报(2017);Structuralinsights into the activation of GLP-1R by a smallmoleculeagonist,C...
2023年9月29日,硕迪生物(Structure Therapeutics)公布小分子GLP-1R激动剂GSBR-1290 1b期临床最新数据。 受此消息影响,硕迪生物股价当天大涨35%,市值达到19.3亿美元。 GSBR-1290 1b期临床MAD(多剂量)实验设计如下,入组标准为BMI在27以上成年人。 GSBR-1290设置3个剂量组,分别为30mg、60mg、90mg,另外一组为安...