GLP-1 effects are mediated through binding to the GLP-1 receptor (GLP-1R), a class B G-protein-coupled receptor (GPCR) that signals primarily through the stimulatory G protein G. Class B GPCRs are important therapeutic targets; however, our understanding of their mechanism of action is ...
12月18日,硕迪生物(StructureTherapeutics)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=54)中分别有10、26、18例受试者每日1次接受...
Glucagon-like peptide 1 (GLP-1) regulates glucose homeostasis through the control of insulin release from the pancreas. GLP-1 peptide agonists are efficacious drugs for the treatment of diabetes. To gain insight into the molecular mechanism of action of GLP-1 peptides, here we report the crysta...
Identification of the receptor-bound conformation of GLP-1, because it is a flexible peptide, required constraint of the peptide backbone into a predetermined 3D structure. Constraint was achieved by the introduction of disulfide bonds and specific side chain-side chain cross-links. The biological ...
The polysaccharide containing selenium in Ganoderma lucidum (SeGLP 1) was isolated through water, lye and alcohol extraction ,dialysis, deproteining with Sevage method and purifying by chromatography of DEAE cellulose column. And SeGLP 1 was identified to be a homogeneous fraction with Sephadex G ...
硕迪生物公布1b期临床数据。股价大涨35%! 2023年9月29日,StructureTherapeutics(硕迪生物)公布了其GLP-1R激动剂GSBR-1290的1b期多递增剂量(MAD)研究结果。 GSBR-1290是一款口服小分子GLP-1RA,正在开发用于治疗II型糖尿病和肥胖患者。 2022年9月,GSBR-1290完成了I期单次递增剂量(SAD)研究,时隔一年后多递增剂量...
D'Alessio, D.et al. Fasting and postprandial concentrations of GLP-1 in intestinal lymph and portal plasma: evidence for selective release of GLP-1 in the lymph system.Am. J. Physiol. Regul. Integr. Comp. Physiol.293, R2163–R2169 (2007). ...
GSBR-1290 is an orally-available, small molecule agonist of the GLP-1 receptor, a validated drug target for the treatment of type 2 diabetes (T2DM) and obesity. The Company completed its Phase 1 single ascending dos...
L. Structure-Activity and Protraction Relationship of Long-Acting Glucagon-like Peptide-1 Derivatives: Importance of Fatty Acid Length, Polarity, and ... K Madsen,LB Knudsen,H Agersoe 被引量: 0发表: 0年 Design,Synthesis and Structure-Activity Relationship of the Novel Long-acting GLP-1 Derivat...
Activation of the GLP-1 receptor by a non-peptidic agonist.DOI: 10.1038/s41586-019-1902-z More and more, researchers turn to cryo-electron microscopy (cryo-EM) to gain insights into the structure and function of small molecules in complex with theirdrug discovery targets. One promising area ...