2024年2月13日 · Here, we report cryo-electron microscopy structures of the human GLP-1 receptor (GLP-1R), GCG receptor (GCGR), and GIP receptor (GIPR) in complex with G s proteins without the presence of cognate...

2023年6月15日 · 肠促胰岛素主要包括GIP和胰高血糖素样肽-1（GLP-1，glucagon-likepeptide-1），它们分别通过作用于β细胞相应受体GIPR和 GLP-1R，进而调控β细胞分化增殖、胰岛素合成与分泌等，发挥其主要作用（图2） [6]。

2022年1月6日 · A synthetic peptide triagonist (SAR441255) of glucagon-like peptide 1 (GLP1), glucose-dependent insulinotropic polypeptide (GIP) and glucagon receptors has been reported to be effective for weight...

Here, we report that GLP-1 augments glucose-dependent rises in NAD (P)H autofluorescence in both βTC3 insulinoma cells and islets in a manner consistent with post-translational activation of glucokinase (GCK). GLP-1 treatment increased GCK activity and enhanced GCK S …

2024年12月25日 · GCKR (Glucokinase Regulator) is a Protein Coding gene. Diseases associated with GCKR include Fasting Plasma Glucose Level Quantitative Trait Locus 5 and Hypercholesterolemia, Familial, 1. Among its related pathways are Transport of the SLBP independent Mature mRNA and Glycolysis (REACTOME).

2011年5月13日 · Here, we report that GLP-1 augments glucose-dependent rises in NAD (P)H autofluorescence in both βTC3 insulinoma cells and islets in a manner consistent with post-translational activation of glucokinase (GCK). GLP-1 treatment increased GCK activity and enhanced GCK S-nitrosylation in βTC3 cells.

2020年6月23日 · 研究了12个具有MODY2血糖特点的中国家系，对先证者及其亲属进行GCK基因突变筛查。 体外构建野生型和突变型葡萄糖激酶，测定酶的动力学参数和热稳定性。 在12个家系中，共发现11个GCK基因突变（R43C, T168A, K169N, R191W, Y215X, E221K, M235T, R250H, W257X, G261R and A379E）和1个意义不确定的变异（R275H）。 其中R191W同时出现在两个无关的家系中。

On April 15, 2014, the US Food and Drug Administration (FDA) approved albiglutide (Tanzeum; GlaxoSmithKline), a GLP-1 receptor agonist subcutaneous injection, as an adjunct to diet and exercise to improve glycemic control in adult patients with type 2 diabetes mellitus. 8 Commenting on the approval of albiglutide, Curtis Rosebraugh, MD, MPH, Dir...

2023年3月1日 · GLP-1的发现开拓了糖尿病治疗的新靶点，GLP-1 RA 不仅可以降糖，还带来心血管、血压、血脂、体重多重临床获益，GLP-1R激动剂的新适应症也在临床前和临床中积极拓展中，GLP-1R激动剂利拉鲁肽，索马鲁肽、艾塞那肽和利司那肽已获FDA批准或正在试验中用于治疗2型糖尿病，目前正在研究以确定它们在治疗神经退行性疾病方面的潜在疗效。 表2总结了其中部分临床试验，红色或绿色的药物已被批准用于代谢性疾病的治疗，蓝色的为正在进行代谢性疾病 …

RNA interference experiments indicate that GCK is required for the maximal activation of JNK by LPS, lipid A, poly (IC), and, to a lesser extent, IL-1 and engagement of CD40. GCK is ubiquitinated in situ and stabilized by inhibitors of the proteasome, indicating that GCK is subject to proteasomal turnover.