Manandhar Bikash, Ahn Jung-Mo
Department of Chemistry, University of Texas at Dallas , Richardson, Texas 75080, United States.
J Med Chem. 2015 Feb 12;58(3):1020-37. doi: 10.1021/jm500810s. Epub 2014 Nov 13.
Glucagon-like peptide-1 (GLP-1) is an incretin that plays important physiological roles in glucose homeostasis. Produced from intestine upon food intake, it stimulates insulin secretion and keeps pancreatic β-cells healthy and proliferating. Because of these beneficial effects, it has attracted a great deal of attention in the past decade, and an entirely new line of diabetic therapeutics has emerged based on the peptide. In addition to the therapeutic applications, GLP-1 analogs have demonstrated a potential in molecular imaging of pancreatic β-cells; this may be useful in early detection of the disease and evaluation of therapeutic interventions, including islet transplantation. In this Perspective, we focus on GLP-1 analogs for their studies on improvement of biological activities, enhancement of metabolic stability, investigation of receptor interaction, and visualization of the pancreatic islets.
胰高血糖素样肽-1(GLP-1)是一种肠促胰岛素,在葡萄糖稳态中发挥重要的生理作用。进食后由肠道产生,它刺激胰岛素分泌并维持胰腺β细胞的健康和增殖。由于这些有益作用,在过去十年中它引起了广泛关注,并且基于该肽出现了全新的糖尿病治疗方法。除了治疗应用外,GLP-1类似物在胰腺β细胞的分子成像中也显示出潜力;这可能有助于疾病的早期检测和治疗干预的评估,包括胰岛移植。在这篇观点文章中,我们重点关注GLP-1类似物在改善生物活性、增强代谢稳定性、研究受体相互作用以及胰腺胰岛可视化方面的研究。