California Institute for Biomedical Research , La Jolla , California 92037 , United States.
Department of Chemistry, The Skaggs Institute for Chemical Biology , The Scripps Research Institute , La Jolla , California 92037 , United States.
J Med Chem. 2018 Apr 12;61(7):3218-3223. doi: 10.1021/acs.jmedchem.7b00768. Epub 2018 Mar 23.
Glucagon-like peptide 2 (GLP-2) is a hormone that has been shown to stimulate intestinal growth and attenuate intestinal inflammation. Despite being efficacious in a variety of animal models of disease, its therapeutic potential is hampered by the short half-life in vivo. We now describe a highly potent, stapled long-acting GLP-2 analog, peptide 10, that has a more than 10-fold longer half-life than teduglutide and improved intestinotrophic and anti-inflammatory effects in mouse models of DSS-induced colitis.
胰高血糖素样肽 2（GLP-2）是一种激素，已被证明可刺激肠道生长并减轻肠道炎症。尽管在多种疾病的动物模型中均有效，但由于其体内半衰期短，其治疗潜力受到限制。我们现在描述了一种高效、订书钉式长效 GLP-2 类似物，即肽 10，其半衰期比 teduglutide 长 10 多倍，并且在 DSS 诱导的结肠炎小鼠模型中具有更好的肠营养和抗炎作用。
